Notoginsenoside T5

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Notoginsenoside T5 

Notoginsenoside T5 是一种 dammarane 61 glycoside. Notoginsenoside T5 是从 P. 62 notoginseng 的根皂苷酸性脱糖基中分离出来的。

Notoginsenoside T5

Notoginsenoside T5 Chemical Structure

CAS No. : 769932-34-5

规格 是否有货
5 mg 询价
10 mg 询价
25 mg 询价

* Please select Quantity before adding items.

生物活性

Notoginsenoside T5 is a dammarane 61 glycoside. Notoginsenoside T5 is isolated from the acidic deglycosylation of saponins from the roots of P. 62 notoginseng[1].

分子量

752.97

Formula

C41H68O12

CAS 号

769932-34-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Wang RF, et al. Chemical transformation and target preparation of saponins in stems and leaves of Panax notoginseng. J Ginseng Res. 2018;42(3):270-276.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Notoginsenoside T5

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Notoginsenoside T5 

Notoginsenoside T5 是一种 dammarane 61 glycoside. Notoginsenoside T5 是从 P. 62 notoginseng 的根皂苷酸性脱糖基中分离出来的。

Notoginsenoside T5

Notoginsenoside T5 Chemical Structure

CAS No. : 769932-34-5

规格 是否有货
5 mg 询价
10 mg 询价
25 mg 询价

* Please select Quantity before adding items.

生物活性

Notoginsenoside T5 is a dammarane 61 glycoside. Notoginsenoside T5 is isolated from the acidic deglycosylation of saponins from the roots of P. 62 notoginseng[1].

分子量

752.97

Formula

C41H68O12

CAS 号

769932-34-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Wang RF, et al. Chemical transformation and target preparation of saponins in stems and leaves of Panax notoginseng. J Ginseng Res. 2018;42(3):270-276.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Notoginsenoside T5

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Notoginsenoside T5 

Notoginsenoside T5 是一种 dammarane 61 glycoside. Notoginsenoside T5 是从 P. 62 notoginseng 的根皂苷酸性脱糖基中分离出来的。

Notoginsenoside T5

Notoginsenoside T5 Chemical Structure

CAS No. : 769932-34-5

规格 是否有货
5 mg 询价
10 mg 询价
25 mg 询价

* Please select Quantity before adding items.

生物活性

Notoginsenoside T5 is a dammarane 61 glycoside. Notoginsenoside T5 is isolated from the acidic deglycosylation of saponins from the roots of P. 62 notoginseng[1].

分子量

752.97

Formula

C41H68O12

CAS 号

769932-34-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Wang RF, et al. Chemical transformation and target preparation of saponins in stems and leaves of Panax notoginseng. J Ginseng Res. 2018;42(3):270-276.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

UU-T02

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

UU-T02 

UU-T02 是一种新型强效的 β-Catenin/T-cell factor 蛋白互作的选择性小分子抑制剂 (β-catenin/Tcf PPI)Ki 为 1.36 μM。UU-T02 抑制典型 Wnt 信号的传导和结直肠癌细胞的生长。

UU-T02

UU-T02 Chemical Structure

CAS No. : 1500080-17-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

UU-T02 is a novel potent, selective small-molecule inhibitor of β-Catenin/T-cell factor protein-protein interaction (β-catenin/Tcf PPI) with a Ki of 1.36 μM[1]. UU-T02 inhibits canonical Wnt signaling and the growth of colorectal cancer cells[2].

IC50 & Target

Ki: 1.36 μM (β-catenin/Tcf PPI)[1].
IC50: 6.3 μM (β-catenin/Tcf4), 680 μM (β-catenin/E-cadherin) , 210 μM (β-catenin/APC-R3)[2].

体外研究
(In Vitro)

UU-T02 displays Ki values of 1.4 μM and 1.3 μM for β-catenin/Tcf PPI in FP assay and in AlphaScreen assay, respectively[2].
UU-T02 inhibits β-catenin/Tcf4, β-catenin/E-cadherin, β-catenin/APC-R3, with the IC50 of 6.3, 680, 210 μM,respectively[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

665.09

Formula

C33H33ClN4O9

CAS 号

1500080-17-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Huang Z, et al. Targeting the Tcf4 G13ANDE17 binding site to selectively disrupt β-catenin/T-cell factor protein-protein interactions. ACS Chem Biol. 2014;9(1):193-201.

    [2]. Catrow JL, et al. Discovery of Selective Small-Molecule Inhibitors for the β-Catenin/T-Cell Factor Protein-Protein Interaction through the Optimization of the Acyl Hydrazone Moiety. J Med Chem. 2015;58(11):4678-4692.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

UU-T02

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

UU-T02 

UU-T02 是一种新型强效的 β-Catenin/T-cell factor 蛋白互作的选择性小分子抑制剂 (β-catenin/Tcf PPI)Ki 为 1.36 μM。UU-T02 抑制典型 Wnt 信号的传导和结直肠癌细胞的生长。

UU-T02

UU-T02 Chemical Structure

CAS No. : 1500080-17-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

UU-T02 is a novel potent, selective small-molecule inhibitor of β-Catenin/T-cell factor protein-protein interaction (β-catenin/Tcf PPI) with a Ki of 1.36 μM[1]. UU-T02 inhibits canonical Wnt signaling and the growth of colorectal cancer cells[2].

IC50 & Target

Ki: 1.36 μM (β-catenin/Tcf PPI)[1].
IC50: 6.3 μM (β-catenin/Tcf4), 680 μM (β-catenin/E-cadherin) , 210 μM (β-catenin/APC-R3)[2].

体外研究
(In Vitro)

UU-T02 displays Ki values of 1.4 μM and 1.3 μM for β-catenin/Tcf PPI in FP assay and in AlphaScreen assay, respectively[2].
UU-T02 inhibits β-catenin/Tcf4, β-catenin/E-cadherin, β-catenin/APC-R3, with the IC50 of 6.3, 680, 210 μM,respectively[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

665.09

Formula

C33H33ClN4O9

CAS 号

1500080-17-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Huang Z, et al. Targeting the Tcf4 G13ANDE17 binding site to selectively disrupt β-catenin/T-cell factor protein-protein interactions. ACS Chem Biol. 2014;9(1):193-201.

    [2]. Catrow JL, et al. Discovery of Selective Small-Molecule Inhibitors for the β-Catenin/T-Cell Factor Protein-Protein Interaction through the Optimization of the Acyl Hydrazone Moiety. J Med Chem. 2015;58(11):4678-4692.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

UU-T02

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

UU-T02 

UU-T02 是一种新型强效的 β-Catenin/T-cell factor 蛋白互作的选择性小分子抑制剂 (β-catenin/Tcf PPI)Ki 为 1.36 μM。UU-T02 抑制典型 Wnt 信号的传导和结直肠癌细胞的生长。

UU-T02

UU-T02 Chemical Structure

CAS No. : 1500080-17-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

UU-T02 is a novel potent, selective small-molecule inhibitor of β-Catenin/T-cell factor protein-protein interaction (β-catenin/Tcf PPI) with a Ki of 1.36 μM[1]. UU-T02 inhibits canonical Wnt signaling and the growth of colorectal cancer cells[2].

IC50 & Target

Ki: 1.36 μM (β-catenin/Tcf PPI)[1].
IC50: 6.3 μM (β-catenin/Tcf4), 680 μM (β-catenin/E-cadherin) , 210 μM (β-catenin/APC-R3)[2].

体外研究
(In Vitro)

UU-T02 displays Ki values of 1.4 μM and 1.3 μM for β-catenin/Tcf PPI in FP assay and in AlphaScreen assay, respectively[2].
UU-T02 inhibits β-catenin/Tcf4, β-catenin/E-cadherin, β-catenin/APC-R3, with the IC50 of 6.3, 680, 210 μM,respectively[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

665.09

Formula

C33H33ClN4O9

CAS 号

1500080-17-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Huang Z, et al. Targeting the Tcf4 G13ANDE17 binding site to selectively disrupt β-catenin/T-cell factor protein-protein interactions. ACS Chem Biol. 2014;9(1):193-201.

    [2]. Catrow JL, et al. Discovery of Selective Small-Molecule Inhibitors for the β-Catenin/T-Cell Factor Protein-Protein Interaction through the Optimization of the Acyl Hydrazone Moiety. J Med Chem. 2015;58(11):4678-4692.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

SMTIN-T140

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SMTIN-T140 

SMTIN-T140 (化合物 6a) 是一种有效的 TRAP1 (肿瘤坏死因子受体相关蛋白 1) 抑制剂,其 IC50 为 1.646 μM。SMTIN-T140 具有抗癌活性。SMTIN-T140 导致线粒体功能障碍,增加线粒体 ROS 生成,并激活 AMPK。在 PC3 前列腺癌细胞异种移植的小鼠模型中,SMTIN-T140 能有效抑制肿瘤生长,且体内毒性不明显。

SMTIN-T140

SMTIN-T140 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SMTIN-T140 (compound 6a) is a potent TRAP1 (tumor-necrosis-factor-receptor associated protein 1) inhibitor, with an IC50 of 1.646 μM. SMTIN-T140 shows anticancer activity. SMTIN-T140 leads to mitochondrial dysfunction, increases mitochondrial ROS production and activates AMPK. SMTIN-T140 potently suppressed tumor growth without any noticeable in vivo toxicity in a mouse model xenografted with PC3 prostate cancer cells[1].

IC50 & Target

IC50: 1.646 ± 0.024 μM (TRAP1)[1]

分子量

718.02

Formula

C36H34BrClFN5OP+

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Yang S, et al. Triphenylphosphonium conjugation to a TRAP1 inhibitor, 2-amino-6-chloro-7,9-dihydro-8H-purin-8-one increases antiproliferative activity. Bioorg Chem. 2022 May 20;126:105856.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

HDAC3-IN-T247

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

HDAC3-IN-T247 

HDAC3-IN-T247 是一种有效的选择性 HDAC3 (组蛋白去乙酰化酶 3) 抑制剂,其 IC50 为 0.24 μM。HDAC3-IN-T247 诱导 HCT116 细胞选择性增加 NF-κB 乙酰化。HDAC3-IN-T247 具有抗癌和抗病毒活性。HDAC3-IN-T247 能抑制癌细胞生长,激活潜伏在 HIV 感染细胞中的 HIV 基因表达。

HDAC3-IN-T247

HDAC3-IN-T247 Chemical Structure

CAS No. : 1451042-18-4

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

HDAC3-IN-T247 is a potent and selective HDAC3 (histone deacetylase 3) inhibitor, with an IC50 of 0.24 µM. HDAC3-IN-T247 induces a selective increase of NF-κB acetylation in HCT116 cells. HDAC3-IN-T247 shows anticancer and antiviral activity. HDAC3-IN-T247 inhibits growth of cancer cells, and activates HIV gene expression in latent HIV-infected cells[1].

IC50 & Target

HDAC3

0.24 μM (IC50)

HDAC1

19 μM (IC50)

HDAC4

>100 μM (IC50)

HDAC6

>100 μM (IC50)

HDAC8

>100 μM (IC50)

分子量

389.47

Formula

C21H19N5OS

CAS 号

1451042-18-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Suzuki T, et al. Identification of highly selective and potent histone deacetylase 3 inhibitors using click chemistry-based combinatorial fragment assembly. PLoS One. 2013 Jul 16;8(7):e68669.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

T0901317

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

T0901317  纯度: 99.91%

T0901317 是口服有效且高度选择性的 LXR 激动剂,对 LXRα 的 EC50 为 20 nM。T0901317 激活 FXREC50 为 5 μM。T0901317 是 RORαRORγ 双重反向激动剂,Ki 值分别为 132 nM 和 51 nM。T0901317 诱导细胞凋亡 (apoptosis),并抑制低密度脂蛋白 (LDL) 受体缺失小鼠动脉粥样硬化的发展。

T0901317

T0901317 Chemical Structure

CAS No. : 293754-55-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥660 In-stock
10 mg ¥600 In-stock
50 mg ¥1200 In-stock
100 mg ¥1950 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

T0901317 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • Orally Active Compound Library
  • Chemical Probe Library
  • Transcription Factor Targeted Library
  • Lipid Metabolism Compound Library

生物活性

T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα[1]. T0901317 activates FXR with an EC50 of 5 μM[2]. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively[3]. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice[4][5].

IC50 & Target

EC50: 20 nM (LXRα) and 5 μM (FXR)[1][2]
Ki: 132 nM (RORα) and 51 nM (RORγ)[3]

体外研究
(In Vitro)

T0901317 (5-50 μM; 72 hours) significantly inhibits cellular proliferation in CaOV3, SKOV3, A2780 (human ovarian carcinoma cell lines) in a dose-dependent and time-dependent manner[5].
T0901317 (10 μM; 24-72 hours) decreases the percentage of cells in S phase and increases the percentage of cells in the G0/G1 phase, indicating a cell cycle arrest at the G1-S checkpoint. The percentage of cells in G0/G1 phase increases in a time-dependent manner[5].
T0901317 (10-40 μM; 24 hours ) results in a significant increase of cells in early apoptosis[5].
T0901317 (5-40 μM; 48 hours) results in an increase of p21 and p27 protein expression in a dose-dependent manner after 48 hours[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[5]

Cell Line: A2780, CaOV3 and SKOV3 ovarian cancer cell lines
Concentration: 5, 10, 20, 40 or 50 μM
Incubation Time: 72 hours
Result: Inhibited cellular proliferation in all cell lines in a dose-dependent and time-dependent manner.

Cell Cycle Analysis[5]

Cell Line: A2780, CaOV3 and SKOV3 cells
Concentration: 10 μM
Incubation Time: 24, 48 or 72 hours
Result: Decreased the percentage of cells in S phase and increased the percentage of cells in the G0/G1 phase.

Apoptosis Analysis[5]

Cell Line: CaOV3 cells
Concentration: 10 to 40 μM
Incubation Time: 24 hours
Result: Resulted in a significant increase of cells in early apoptosis.

Western Blot Analysis[5]

Cell Line: CaOV3 cells
Concentration: 5 to 40 μM
Incubation Time: 48 hours
Result: Resulted in an increase of p21 and p27 protein expression in a dose-dependent manner.

体内研究
(In Vivo)

T0901317 (10 mg/kg/day; orally; for 12 weeks) inhibits the progression of atherosclerosis[5].
T0901317 (i.p.; 50 mg/kg; twice weekly for 7 days) can protect male C57BL/6 mice from high fat diet-induced obesity and insulin resistance[6].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8- to 10-week-old LDL receptor null mice[5]
Dosage: 10 mg/kg
Administration: Orally; daily; for 12 weeks
Result: Inhibited the progression of atherosclerosis.

分子量

481.33

Formula

C17H12F9NO3S

CAS 号

293754-55-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (207.76 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0776 mL 10.3879 mL 20.7758 mL
5 mM 0.4155 mL 2.0776 mL 4.1552 mL
10 mM 0.2078 mL 1.0388 mL 2.0776 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3 mg/mL (6.23 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (6.23 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3 mg/mL (6.23 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (6.23 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (6.23 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (6.23 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 4.

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: 2.5 mg/mL (5.19 mM); Suspended solution; Need ultrasonic

  • 5.

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. J R Schultz, et al. Role of LXRs in Control of Lipogenesis. Genes Dev. 2000 Nov 15;14(22):2831-8.

    [2]. Keith A Houck, et al. T0901317 Is a Dual LXR/FXR Agonist. Mol Genet Metab. Sep-Oct 2004;83(1-2):184-7.

    [3]. Naresh Kumar, et al. The Benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] Is a Novel Retinoic Acid Receptor-Related Orphan Receptor-Alpha/Gamma Inverse Agonist. Mol Pharmacol. 2010 Feb;77(2):228-36.

    [4]. Rough JJ, et al. Anti-proliferative effect of LXR agonist T0901317 in ovarian carcinoma cells. J Ovarian Res. 2010 May 26;3:13.

    [5]. Todd G Kirchgessner, et al. Beneficial and Adverse Effects of an LXR Agonist on Human Lipid and Lipoprotein Metabolism and Circulating Neutrophils. Cell Metab. 2016 Aug 9;24(2):223-33.

    [6]. Mingming Gao, et al. The Liver X Receptor Agonist T0901317 Protects Mice From High Fat Diet-Induced Obesity and Insulin Resistance. AAPS J. 2013 Jan;15(1):258-66.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

T0070907

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

T0070907  纯度: 99.98%

T0070907是有效的 PPARγ 拮抗剂,Ki值为1 nM。

T0070907

T0070907 Chemical Structure

CAS No. : 313516-66-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥500 In-stock
5 mg ¥372 In-stock
10 mg ¥558 In-stock
50 mg ¥2009 In-stock
100 mg ¥3832 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

T0070907 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Oxygen Sensing Compound Library
  • Transcription Factor Targeted Library
  • Lipid Metabolism Compound Library

生物活性

T0070907 is a potent PPARγ antagonist with a Ki of 1 nM.

IC50 & Target[4]

PPARγ

1 nM (Ki)

PPARδ

1.8 μM (Ki)

PPARα

0.85 μM (Ki)

体外研究
(In Vitro)

T0070907 (50 μM) pre-treatment impairs repair of IR-induced DNA DSBs in both ME-180 and SiHa cells treated with irradiated (4 Gy). T0070907 (0-50 μM) significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells[1]. T0070907 (50 μM) treatment reduces the levels of α- and β-tubulin protein in a time-dependent manner, decreases the synthesis of DNA, and prevents the radiation-induced alterations in the cell cycle regulatory proteins of ME180 and SiHa cells[2]. T0070907 (10 µM) has cytotoxicity in an adipocyte-specific and PPARγ-independent manner. T0070907 increases oxidative stress in immature adipocytes[3]. T0070907 (1 μM) blocks the induction of adipogenesis by various treatments of the adipogenic cell line 3T3-L1. T0070907 covalently modifies PPAR on cysteine 313 in helix 3 of human PPAR 2[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

277.66

Formula

C12H8ClN3O3

CAS 号

313516-66-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (225.10 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6015 mL 18.0076 mL 36.0153 mL
5 mM 0.7203 mL 3.6015 mL 7.2031 mL
10 mM 0.3602 mL 1.8008 mL 3.6015 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (3.60 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (3.60 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (3.60 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (3.60 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (3.60 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (3.60 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. An Z, et al. T0070907 inhibits repair of radiation-induced DNA damage by targeting RAD51. Toxicol In Vitro. 2016 Dec;37:1-8

    [2]. An Z, et al. T0070907, a PPAR γ inhibitor, induced G2/M arrest enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. Reprod Sci. 2014 Nov;21(11):1352-61.

    [3]. Kawahara A, et al. Peroxisome proliferator-activated receptor γ (PPARγ)-independent specific cytotoxicity against immature adipocytes induced by PPARγ antagonist T0070907. Biol Pharm Bull. 2013;36(9):1428-34

    [4]. Lee G, et al. T0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities. J Biol Chem. 2002 May 31;277(22):19649-57. Epub 2002 Mar 4

Kinase Assay
[4]

To determine the binding affinity of T0070907 to the PPARs, scintillation proximity assay (SPA) is performed with the following modifications. A 90 μL reaction contains SPA buffer (10 mM K2HPO4, 10 mM KH2PO4, 2 mM EDTA, 50 mM NaCl, 1 mM dithiothreitol, 2 mM CHAPS, 10% (v/v) glycerol, pH 7.1), 50 ng of GST-PPAR (or 150 ng of GST-PPAR), 5 nM 3H-labeled radioligands, and 5 μL of T0070907 in Me2SO. After incubation for 1 h at room temperature, 10 μL of polylysine-coated SPA beads (at 20 mg/mL in SPA buffer) are added, and the mixture is incubated for 1 h before reading in Packard Topcount. [3H]Rosiglitazone is used for PPAR, and [3H]GW2433 is used for PPAR and PPAR.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. An Z, et al. T0070907 inhibits repair of radiation-induced DNA damage by targeting RAD51. Toxicol In Vitro. 2016 Dec;37:1-8

    [2]. An Z, et al. T0070907, a PPAR γ inhibitor, induced G2/M arrest enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. Reprod Sci. 2014 Nov;21(11):1352-61.

    [3]. Kawahara A, et al. Peroxisome proliferator-activated receptor γ (PPARγ)-independent specific cytotoxicity against immature adipocytes induced by PPARγ antagonist T0070907. Biol Pharm Bull. 2013;36(9):1428-34

    [4]. Lee G, et al. T0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities. J Biol Chem. 2002 May 31;277(22):19649-57. Epub 2002 Mar 4

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Epoxomicin(Synonyms: 环氧酶素; BU-4061T)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Epoxomicin (Synonyms: 环氧酶素; BU-4061T) 纯度: 98.81%

Epoxomicin (BU-4061T) 是一种含环氧酮的天然产物,是一种有效的,选择性的和不可逆的蛋白酶体 (proteasome) 抑制剂。Epoxomicin 与蛋白酶体的LMP7,X,MECL1 和 Z 催化亚基共价结合,并有效地主要抑制类胰凝乳蛋白酶的活性。Epoxomicin 可以穿越血脑屏障,并具有很强的抗肿瘤和抗炎活性。

Epoxomicin(Synonyms: 环氧酶素; BU-4061T)

Epoxomicin Chemical Structure

CAS No. : 134381-21-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5370 In-stock
100 μg ¥800 In-stock
1 mg ¥1600 In-stock
5 mg ¥4400 In-stock
10 mg ¥8000 In-stock
20 mg ¥12500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Epoxomicin 相关产品

相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus

生物活性

Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity[1][2][3][4][5].

IC50 & Target

Proteasome[1]

体外研究
(In Vitro)

Epoxomicin shows quite potent cytotoxicities against all of the cells tested. Epoxomicin inhibits the cells growth of B16-F10, HCT116, Moser, P388 and K562 cells of IC50 values of 0.002 μg/mL, 0.005 μg/mL, 0.044 μg/mL, 0.002 μg/mL and 0.037 μg/mL[1].
Epoxomicin has antiproliferative activity with an IC50 of 4 nM in EL4 lymphoma cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Epoxomicin (0.063-1 mg/kg; intraperitoneal injection; once daily; for 9 days; male BDFX mice) treatment shows significant antitumor effect with the minimumeffective dose of 0.13mg/kg/day[1].
Epoxomicin also effectively inhibits NF-κB activation in vitro and potently blocks in vivo inflammation in the murine ear edema assay[3].
Epoxomicin is injected into adult rats over a period of 2 weeks. After a latency of 1 to 2 weeks, animals developed progressive Parkinsonism with bradykinesia, rigidity, tremor, and an abnormal posture. Postmortem analyses shows striatal dopamine depletion and dopaminergic cell death with apoptosis in the substantia nigra pars compacta[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BDFX mice with B16 melanoma[1]
Dosage: 0.063 mg/kg, 0.13 mg/kg, 0.25 mg/kg, 0.5 mg/kg, 1 mg/kg
Administration: Intraperitoneal injection; once daily; for 9 days
Result: Exhibited strong therapeutic activity against B16 melanoma.

分子量

554.72

Formula

C28H50N4O7

CAS 号

134381-21-8

中文名称

环氧酶素

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (180.27 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8027 mL 9.0136 mL 18.0271 mL
5 mM 0.3605 mL 1.8027 mL 3.6054 mL
10 mM 0.1803 mL 0.9014 mL 1.8027 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.51 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.51 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.51 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.51 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.51 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.51 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Hanada M, et al. Epoxomicin, a new antitumor agent of microbial origin. J Antibiot (Tokyo). 1992 Nov;45(11):1746-52.

    [2]. Kim KB, et al. Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency. Bioorg Med Chem Lett. 1999 Dec 6;9(23):3335-40.

    [3]. Meng L, et al. Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity. Proc Natl Acad Sci U S A. 1999 Aug 31;96(18):10403-8.

    [4]. McNaught KS, et al. Systemic exposure to proteasome inhibitors causes a progressive model of Parkinson’s disease. Ann Neurol. 2004 Jul;56(1):149-62.

    [5]. Garrett IR, et al. Selective inhibitors of the osteoblast proteasome stimulate bone formation in vivo and in vitro. J Clin Invest. 2003 Jun;111(11):1771-82.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

OSU-T315

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

OSU-T315  纯度: 99.21%

OSU-T315 是整联蛋白连接激酶 (ILK) 的抑制剂 (IC50=0.6 μM), 通过去磷酸化 AKT-Ser473 和其他 ILK 靶标 (GSK-3β和肌球蛋白轻链) 抑制 PI3K/AKT 信号传导。 OSU-T315 阻止 AKT 转位到脂筏消除 AKT 的活化,并以 ILK 非依赖性方式触发 Caspase 依赖性细胞凋亡 (Apoptosis)。OSU-T315 通过自噬 (Autophagy) 和凋亡 (Apoptosis) 导致细胞死亡。

OSU-T315

OSU-T315 Chemical Structure

CAS No. : 2070015-22-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3520 In-stock
5 mg ¥3000 In-stock
10 mg ¥5000 In-stock
50 mg ¥13000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

OSU-T315 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library

生物活性

OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain)[1]. OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner[2]. OSU-T315 causes cell death through apoptosis and autophagy[1].

IC50 & Target

IC50: 0.6μM; Integrin-linked kinase (ILK) inhibitor[1]

体外研究
(In Vitro)

OSU-T315 (Compound 22; 0-5 μM; 24 hours) exhibits high in vitro potency against a panel of prostate and breast cancer cell lines with a IC50 range of 1-2.5 μM[1].
OSU-T315 (0-2.5 μM; 24 hours) can reduce YB-1, HER2, and EGFR expression; shows a modest suppressive effect on phosphorylated S6 levels, exhibits dose-dependent suppressive effects on the levels of phospho-ERK1/2 and phospho-p38, while that of phospho-JNK remains unaltered in PC-3 cell[1].
OSU-T315 (0-4 μM; 24 hours) causes autophagy through ILK inhibition[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis [1]

Cell Line: PC-3 cells; MDA-MB-231 cells
Concentration: 1 μM, 2 μM, 3 μM, 4 μM; 0.5 μM, 1 μM, 1.5 μM, 2 μM, 2.5 μM
Incubation Time: 24 hours
Result: Exhibited a dose-dependent decreasing effect on the phosphorylation of pS6, ERKs, and p38 in PC-3 cells and MDA-MB-231 cells.

Cell Viability Assay [1]

Cell Line: Prostate cancer cells: LNCaP, PC-3; breast cancer cells: MDA-MB-231, MDA-MB-468, SKBR3, MCF-7; PrEC and MEC cells
Concentration: 0-5 μM
Incubation Time: 24 hours
Result: Suppressed cancer cells viability in breast and prostate cancer cells (IC (50), 1-2.5μM).

Apoptosis Analysis[1]

Cell Line: PC-3 cells
Concentration: 1 μM, 2 μM, 3 μM, 4 μM
Incubation Time: 24 hours
Result: Induced accumulation of LC3-II and PARP cleavage.

体内研究
(In Vivo)

OSU-T315 (Oral gavage; 25 mg/kg, 50 mg/kg; single daily; 35 days) has a suppressive effect of on PC-3 xenograft tumor growth [1].
No other obvious toxicity is observed in mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male NCr athymic nude mice with PC-3 tumor xenografts
Dosage: 25 mg/kg; 50 mg/kg
Administration: Oral gavage; single daily; 35 days
Result: Resulted in suppression of tumor growth relative to the vehicle control after 35 days of treatment (48% and 62% suppression for 25 and 50 mg/kg, respectively).

分子量

533.59

Formula

C30H30F3N5O

CAS 号

2070015-22-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 260 mg/mL (487.27 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8741 mL 9.3705 mL 18.7410 mL
5 mM 0.3748 mL 1.8741 mL 3.7482 mL
10 mM 0.1874 mL 0.9370 mL 1.8741 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (4.07 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (4.07 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (4.07 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (4.07 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Su-Lin Lee,et al Identification and Characterization of a Novel Integrin-Linked Kinase Inhibitor.J Med Chem. 2011 Sep 22; 54(18): 6364–6374

    [2]. Liu TM, et al. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chronic lymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

UT-155

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

UT-155  纯度: 99.91%

UT-155 是一种选择性的、有效的雄激素受体 (AR) 拮抗剂,与 AR-LBD 结合的 Ki 值为 267 nM。

UT-155

UT-155 Chemical Structure

CAS No. : 2031161-35-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3850 In-stock
5 mg ¥3500 In-stock
10 mg ¥5500 In-stock
25 mg ¥11000 In-stock
50 mg ¥17500 In-stock
100 mg ¥27500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

UT-155 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Transcription Factor Targeted Library

生物活性

UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.

IC50 & Target

Ki: 267 nM (AR-LBD)[1].

体外研究
(In Vitro)

UT-155 binds to the AR-LBD at Ki of 267 nM. UT-155 potently inhibits the R1881-induced wildtype AR transactivation with 6-10-fold higher potency than enzalutamide. While UT-155 antagonizes both wildtype and mutant ARs comparably, enzalutamide is weaker by two fold with the W742L mutant AR relative to the wild type AR. Treatment of LNCaP cells with UT-155 inhibits 0.1 nM R1881-induced PSA and FKBP5 gene expression between 10 and 100 nM with 5-10-fold better potency than enzalutamide[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Consistent with the anti-proliferative effects in vitro, UT-155 significantly inhibits the growth of 22RV1 xenograft by 53%, while, as expected, enzalutamide has no effect on the growth of the 22RV1 tumors. Tumor weights and PSA and the expression of AR and AR-SV are significantly lower in UT-155-treated animals[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

405.35

Formula

C20H15F4N3O2

CAS 号

2031161-35-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 130 mg/mL (320.71 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4670 mL 12.3350 mL 24.6700 mL
5 mM 0.4934 mL 2.4670 mL 4.9340 mL
10 mM 0.2467 mL 1.2335 mL 2.4670 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (5.35 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (5.35 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (5.35 mM); Suspended solution

    此方案可获得 ≥ 2.17 mg/mL (5.35 mM,饱和度未知) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (5.35 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (5.35 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Ponnusamy S, et al. Novel Selective Agents for the Degradation of Androgen Receptor Variants to Treat Castration-Resistant Prostate Cancer. Cancer Res. 2017 Nov 15;77(22):6282-6298.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

T56-LIMKi(Synonyms: T5601640)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

T56-LIMKi (Synonyms: T5601640) 纯度: 98.91%

T56-LIMKi是选择性的LIMK2抑制剂。抑制Panc-1细胞生长的IC50值为35.2 μM。

T56-LIMKi(Synonyms: T5601640)

T56-LIMKi Chemical Structure

CAS No. : 924473-59-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥869 In-stock
5 mg ¥790 In-stock
10 mg ¥1370 In-stock
25 mg ¥2800 In-stock
50 mg ¥4800 In-stock
100 mg ¥8100 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

T56-LIMKi 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Targeted Diversity Library

生物活性

T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC50 of 35.2 μM.

IC50 & Target[1]

LIMK2

 

体外研究
(In Vitro)

T56-LIMKi efficiently inhibits the growth of ST88-14, U87, Panc-1 cells, A549 lung cancer cells with IC50 values of 18.3, 7.4, 35.2 and 90 μM, respectively. T56-LIMKi decreases phosphorylated cofilin (p-cofilin) levels and thus inhibits growth of several cancerous cell lines, including those of pancreatic cancer, glioma and schwannoma[1]. It blocks the phosphorylation of cofilin which leads to actin severance and inhibition of tumor cell migration, tumor cell growth, and anchorage-independent colony formation in soft agar. T56-LIMKi (10-50 μM) reduces p-cofilin in a dose-dependent manner in NF1−/−MEFs with an IC50 of 30 μM. Notably, the inhibitor does not affect the amounts of total cofil. 50μM T56-LIMKi causes a statistically significant reduction in the number of cells exhibiting stress fibers[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

T56-LIMKi can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo. Mice treated with T56-LIMKi (60 mg/kg) shows a significant decrease in tumor volume compared to control[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

389.33

Formula

C19H14F3N3O3

CAS 号

924473-59-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 36 mg/mL (92.47 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5685 mL 12.8426 mL 25.6852 mL
5 mM 0.5137 mL 2.5685 mL 5.1370 mL
10 mM 0.2569 mL 1.2843 mL 2.5685 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.42 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Rak R, et al. Novel LIMK2 Inhibitor Blocks Panc-1 Tumor Growth in a mouse xenograft model. Oncoscience. 2014 Jan 1;1(1):39-48. eCollection 2014.

    [2]. Mashiach-Farkash E, et al. Computer-based identification of a novel LIMK1/2 inhibitor that synergizes with salirasib to destabilize the actin cytoskeleton. Oncotarget. 2012 Jun;3(6):629-39.

Cell Assay

T56-LIMKi can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo. Mice treated with T56-LIMKi (60 mg/kg) shows a significant decrease in tumor volume compared to control[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: T56-LIMKi is dissolved in 0.5% carboxymethylcellulose solution. Mice are implanted with xenografted Panc-1 cells. Treatment is started 7 days later. Mice in the two experimental groups are each treated with a daily oral non-toxic dose of T56-LIMKi (30 or 60 mg/kg in gavage) and mice in the control group receives only the vehicle (0.5% CMC) in the gavage[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Rak R, et al. Novel LIMK2 Inhibitor Blocks Panc-1 Tumor Growth in a mouse xenograft model. Oncoscience. 2014 Jan 1;1(1):39-48. eCollection 2014.

    [2]. Mashiach-Farkash E, et al. Computer-based identification of a novel LIMK1/2 inhibitor that synergizes with salirasib to destabilize the actin cytoskeleton. Oncotarget. 2012 Jun;3(6):629-39.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

CU-T12-9

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CU-T12-9  纯度: 99.94%

CU-T12-9 是一种特异性 TLR1/2 激动剂,EC50 为 52.9 nM。CU-T12-9 既激活先天免疫系统,又激活适应性免疫系统。CU-T12-9 选择性激活 TLR1/2 异二聚体而对 TLR2/6 没有作用。CU-T12-9 通过促进 TLR1 和 TLR2 二聚而激活 NF-κB 信号,致使下游 TNF-α,IL-10,和 iNOS 增加,从而提高身体的免疫反应。

CU-T12-9

CU-T12-9 Chemical Structure

CAS No. : 1821387-73-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥877 In-stock
5 mg ¥1100 In-stock
10 mg ¥1800 In-stock
50 mg ¥5500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CU-T12-9 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • NF-κB Signaling Compound Library
  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Antioxidants Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Pyroptosis Compound Library

生物活性

CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS[1].

IC50 & Target[1]

TLR2

52.9 nM (EC50, in HEK-Blue cells)

TLR1

52.9 nM (EC50, in HEK-Blue cells)

体外研究
(In Vitro)

CU-T12-9 directly targets TLR1/2 to initiate downstream signaling. By binding to both TLR1 and TLR2, CU-T12-9 facilitates the TLR1/2 heterodimeric complex formation, which in turn activates the downstream signaling[1].
CU-T12-9 activates the TLR1/2 pathway by inducing NF-κB activation to trigger downstream signaling, such as secreted embryonic alkaline phosphatase (SEAP), NO, and TNF-α[1].
CU-T12-9 (0.39-100 μM; 24 hours) does not produce toxicity up to 100 μM in HEK-Blue hTLR2 and Raw 264.7 cells[1].
CU-T12-9 up-regulates the mRNA levels of TLR1, TLR2, TNF, IL-10, and iNOS. CU-T12-9 (0.1-10 μM) activates TLR1 mRNA and iNOS mRNA after Raw 264.7 cells are treated for 24 hours. CU-T12-9 (0.1-10 μM) activates TLR2 and IL-10 mRNA after Raw 264.7 cells are treated for 2 hours. CU-T12-9 (0.1-10 μM) activates TNF mRNA after Raw 264.7 cells are treated for 8 hours[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: HEK-Blue hTLR2 and Raw 264.7 macrophage cells
Concentration: 0.39, 0.78, 1.56, 3.125, 6.25, 12.5, 25, 50, and 100 μM
Incubation Time: 24 hours
Result: No toxicity was seen up to 100 μM.

RT-PCR[1]

Cell Line: Raw 264.7 cells
Concentration: 0.1, 1, 10 μM
Incubation Time: 24 hours for TLR1 and iNOS mRNA assay
2 hours for TLR2 and IL-10 mRNA assay
8 hours for TNF mRNA assay
Result: Triggered TLR1 mRNA and iNOS mRNA at 24 hours dose-dependently.
Dose-dependent activation of TLR2 mRNA and IL-10 mRNA at 2 hours.
Showed dose-dependent activation of TNF mRNA at 8 hours.

分子量

362.31

Formula

C17H13F3N4O2

CAS 号

1821387-73-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (690.02 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7601 mL 13.8003 mL 27.6007 mL
5 mM 0.5520 mL 2.7601 mL 5.5201 mL
10 mM 0.2760 mL 1.3800 mL 2.7601 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.74 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.74 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Cheng K, et al. Specific activation of the TLR1-TLR2 heterodimer by small-molecule agonists. Sci Adv. 2015;1(3). pii: e1400139.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Batabulin(Synonyms: 巴他布林; T138067)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Batabulin (Synonyms: 巴他布林; T138067) 纯度: 99.91%

Batabulin (T138067) 是一种抗肿瘤剂,可与 β-微管蛋白同种型的子集共价且选择性地结合,从而破坏微管 (microtubule) 聚合。Batabulin 影响细胞形态并导致细胞周期停滞,最终诱导凋亡性细胞死亡。

Batabulin(Synonyms: 巴他布林; T138067)

Batabulin Chemical Structure

CAS No. : 195533-53-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1980 In-stock
5 mg ¥1800 In-stock
10 mg ¥2700 In-stock
50 mg ¥6800 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Batabulin 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Cytoskeleton Compound Library
  • Anti-Lung Cancer Compound Library

生物活性

Batabulin (T138067) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death[1].

IC50 & Target

β-tubulin[1]

体外研究
(In Vitro)

Batabulin (T138067; 30-300 nM; 24 hours; MCF7 cells) treatment shows approximately 25-30% tetraploid (4n) DNA content in cells, indicating an arrest at the G2/M cell-cycle boundary[1].
Batabulin (T138067; 30-300 nM; 24-48 hours; MCF7 cells) treatment shows 25-30% apoptosis. After a 48-hr exposure to 100 nM Batabulin, approximately 50-80% of the cell population is undergoing apoptosis[1].
Batabulin (T138067) binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Covalent modification occurs at a conserved Cys-239 shared by the β1, β2, and β4 tubulin isotypes. Cells exposed to Batabulin become altered in shape, indicating a collapse of the cytoskeleton, and show an increase in chromosomal ploidy[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: MCF7 cells
Concentration: 30 nM, 100 nM and 300 nM
Incubation Time: 24 hours
Result: Showed an arrest at the G2/M cell-cycle boundary.

Apoptosis Analysis[1]

Cell Line: MCF7 cells
Concentration: 30 nM, 100 nM and 300 nM
Incubation Time: 24 hours or 48 hours
Result: 25-30% of cells showed the reduced DNA content characteristic of apoptotic cells.

体内研究
(In Vivo)

Batabulin (T138067; 40 mg/kg; intraperitoneal injection; once per week; on days 5, 12, and 19; male athymic nude mice) treatment impairs the growth of the drug-sensitive CCRF-CEM tumors[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic nude mice (nu/nu) (6-8 week-old, 20-25 g) injected with CCRF-CEM cells[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; once per week; on days 5, 12, and 19
Result: Impaired the growth of the drug-sensitive CCRF-CEM tumors.

Clinical Trial

分子量

371.26

Formula

C13H7F6NO3S

CAS 号

195533-53-0

中文名称

巴他布林

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (269.35 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6935 mL 13.4677 mL 26.9353 mL
5 mM 0.5387 mL 2.6935 mL 5.3871 mL
10 mM 0.2694 mL 1.3468 mL 2.6935 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.73 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.73 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.73 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Shan B, et al. Selective, covalent modification of beta-tubulin residue Cys-239 by T138067, an antitumor agent with in vivo efficacy against multidrug-resistant tumors. Proc Natl Acad Sci U S A. 1999 May 11;96(10):5686-91.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

T025

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

T025  纯度: 98.61%

T025是有口服活性,高选择性的 Cdc2-like 激酶 (CLK) 抑制剂,对CLK1,CLK2,CLK3和CLK4的Kd分别为4.8,0.096,6.5和0.61 nM。

T025

T025 Chemical Structure

CAS No. : 2407433-00-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4950 In-stock
5 mg ¥4500 In-stock
10 mg ¥8000 In-stock
25 mg ¥16500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

T025 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

T025 is an orally available and highly potent Cdc2-like kinase (CLK) inhibitor with Kds of 4.8, 0.096, 6.5, and 0.61 nM for CLK1, CLK2, CLK3, and CLK4, respectively.

IC50 & Target

Kd: 4.8 nM (CLK1), 0.096 nM (CLK2), 6.5 nM (CLK3), 0.61 nM (CLK4)[1]

分子量

382.42

Formula

C21H18N8

CAS 号

2407433-00-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 8.25 mg/mL (21.57 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6149 mL 13.0746 mL 26.1493 mL
5 mM 0.5230 mL 2.6149 mL 5.2299 mL
10 mM 0.2615 mL 1.3075 mL 2.6149 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Iwai K, et al. Anti-tumor efficacy of a novel CLK inhibitor via targeting RNA splicing and MYC-dependent vulnerability. EMBO Mol Med. 2018 Jun;10(6). pii: e8289.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

CLK-IN-T3

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CLK-IN-T3  纯度: 98.40%

CLK-IN-T3 是一种高效,选择性和稳定的 CDC 样激酶 (CLK) 抑制剂,对 CLK1,CLK2 和 CLK3 蛋白激酶的 IC50 分别为 0.67 nM,15 nM 和 110 nM。CLK-IN-T3 具有抗癌活性。

CLK-IN-T3

CLK-IN-T3 Chemical Structure

CAS No. : 2109805-56-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1650 In-stock
5 mg ¥1550 In-stock
10 mg ¥2650 In-stock
25 mg ¥5600 In-stock
50 mg ¥9500 In-stock
100 mg ¥16500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CLK-IN-T3 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Chemical Probe Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

CLK-IN-T3 is a high potent, selective, and stable CDC-like kinase (CLK) inhibitor with IC50s of 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases, respectively. CLK-IN-T3 has anti-cancer activity[1].

IC50 & Target[1]

CLK1

0.67 nM (IC50)

CLK2

15 nM (IC50)

CLK3

110 nM (IC50)

DYRK1A

260 nM (IC50)

DYRK1B

230 nM (IC50)

体外研究
(In Vitro)

CLK-IN-T3 inhibits DYRK1A (IC50=260 nM) and DYRK1B (IC50=230 nM)[1].
CLK-IN-T3 (0.1-10.0 µM; 24 hours) results in mild cell cycle arrest at the G2/M boundary with long-duration (24 h)[1].
CLK-IN-T3 (0.5-1.0 µM; 6 hours) decreases phosphorylation of CLK-targeted SR proteins and CLK proteins increase slightly[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.1, 0.5, 1.0, 5.0, 10.0 µM
Incubation Time: 24 hours
Result: Resulted in mild cell cycle arrest at the G2/M boundary with long-duration (24 h).

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.5, 1.0 μM
Incubation Time: 6 hours
Result: Decreased phosphorylation of CLK-targeted SR proteins and CLK proteins increased slightly.

分子量

482.58

Formula

C28H30N6O2

CAS 号

2109805-56-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 4.83 mg/mL (10.01 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0722 mL 10.3610 mL 20.7220 mL
5 mM 0.4144 mL 2.0722 mL 4.1444 mL
10 mM 0.2072 mL 1.0361 mL 2.0722 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.31 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.31 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Funnell T, et al. CLK-dependent exon recognition and conjoined gene formation revealed with a novel smallmolecule inhibitor. Nat Commun. 2017 Feb 23;8(1):7.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

ILK-IN-2(Synonyms: OSU-T315 analog)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ILK-IN-2 (Synonyms: OSU-T315 analog) 纯度: 98.14%

ILK-IN-2 (OSU-T315 analog) 是一种ILK抑制剂。

ILK-IN-2(Synonyms: OSU-T315 analog)

ILK-IN-2 Chemical Structure

CAS No. : 1333146-24-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2817 In-stock
2 mg ¥1200 In-stock
5 mg ¥2400 In-stock
50 mg ¥4100 询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

ILK-IN-2 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Cytoskeleton Compound Library

生物活性

ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor.

分子量

533.59

Formula

C30H30F3N5O

CAS 号

1333146-24-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (93.70 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8741 mL 9.3705 mL 18.7410 mL
5 mM 0.3748 mL 1.8741 mL 3.7482 mL
10 mM 0.1874 mL 0.9370 mL 1.8741 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (9.37 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (9.37 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (9.37 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (9.37 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Batabulin sodium(Synonyms: T138067 sodium)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Batabulin sodium (Synonyms: T138067 sodium) 纯度: 99.79%

Batabulin sodium (T138067 sodium) 是一种抗肿瘤剂,可与 β-微管蛋白同种型的子集共价且选择性地结合,从而破坏微管 (microtubule) 聚合。Batabulin sodium 影响细胞形态并导致细胞周期停滞,最终诱导凋亡性细胞死亡。

Batabulin sodium(Synonyms: T138067 sodium)

Batabulin sodium Chemical Structure

CAS No. : 195533-98-3

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1980 In-stock
5 mg ¥1800 In-stock
10 mg ¥2700 In-stock
50 mg ¥6800 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Batabulin sodium 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Cytoskeleton Compound Library
  • Anti-Lung Cancer Compound Library
  • Targeted Diversity Library

生物活性

Batabulin sodium (T138067 sodium) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin sodium affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death[1].

IC50 & Target

β-tubulin[1]

体外研究
(In Vitro)

Batabulin (T138067; 30-300 nM; 24 hours; MCF7 cells) treatment shows approximately 25-30% tetraploid (4n) DNA content in cells, indicating an arrest at the G2/M cell-cycle boundary[1].
Batabulin (T138067; 30-300 nM; 24-48 hours; MCF7 cells) treatment shows 25-30% apoptosis. After a 48-hr exposure to 100 nM Batabulin, approximately 50-80% of the cell population is undergoing apoptosis[1].
Batabulin (T138067) binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Covalent modification occurs at a conserved Cys-239 shared by the β1, β2, and β4 tubulin isotypes. Cells exposed to Batabulin become altered in shape, indicating a collapse of the cytoskeleton, and show an increase in chromosomal ploidy[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: MCF7 cells
Concentration: 30 nM, 100 nM and 300 nM
Incubation Time: 24 hours
Result: Showed an arrest at the G2/M cell-cycle boundary.

Apoptosis Analysis[1]

Cell Line: MCF7 cells
Concentration: 30 nM, 100 nM and 300 nM
Incubation Time: 24 hours or 48 hours
Result: 25-30% of cells showed the reduced DNA content characteristic of apoptotic cells.

体内研究
(In Vivo)

Batabulin (T138067; 40 mg/kg; intraperitoneal injection; once per week; on days 5, 12, and 19; male athymic nude mice) treatment impairs the growth of the drug-sensitive CCRF-CEM tumors[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic nude mice (nu/nu) (6-8 week-old, 20-25 g) injected with CCRF-CEM cells[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; once per week; on days 5, 12, and 19
Result: Impaired the growth of the drug-sensitive CCRF-CEM tumors.

Clinical Trial

分子量

393.24

Formula

C13H6F6NNaO3S

CAS 号

195533-98-3

中文名称

巴他布林酸钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 125 mg/mL (317.87 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5430 mL 12.7149 mL 25.4298 mL
5 mM 0.5086 mL 2.5430 mL 5.0860 mL
10 mM 0.2543 mL 1.2715 mL 2.5430 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Shan B, et al. Selective, covalent modification of beta-tubulin residue Cys-239 by T138067, an antitumor agent with in vivo efficacy against multidrug-resistant tumors. Proc Natl Acad Sci U S A. 1999 May 11;96(10):5686-91.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务