Boc-NH-PEG11-OH

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。

Boc-NH-PEG11-OH 

Boc-NH-PEG11-OH 是一种 PROTAC linker,属于 PEG 类。可用于合成 PROTAC 分子。

Boc-NH-PEG11-OH

Boc-NH-PEG11-OH Chemical Structure

CAS No. : 1556847-53-0

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生物活性

Boc-NH-PEG11-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

分子量

601.72

Formula

C27H55NO13

CAS 号

1556847-53-0

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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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IL-17A modulator-1

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。

IL-17A modulator-1 

IL-17A modulator-1 是一种 IL-17A 调节剂,来自专利 WO2021239743+A1,example 9。IL-17A modulator-1 抑制 IL-17A 的生物学效应,pIC50 为 8.2。IL-17A modulator-1 可用于研究与调节 IL-17A 活性相关的疾病或病症,包括具有免疫成分或自身免疫病理的疾病、癌症和神经退行性疾病。

IL-17A modulator-1

IL-17A modulator-1 Chemical Structure

CAS No. : 2748749-29-1

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生物活性

IL-17A modulator-1 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 9. IL-17A modulator-1 inhibits the biological action of IL-17A with a pIC50 of 8.2. IL-17A modulator-1 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders[1].

IC50 & Target[1]

IL-17A

8.2 (pIC50)

分子量

561.63

Formula

C33H31N5O4

CAS 号

2748749-29-1

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]. Barrie Phillip MARTIN, et al. Preparation of amino acid amides as IL-17A modulators. WO2021239743 A1.

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CHR-6494 TFA

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。

CHR-6494 TFA 

CHR-6494 TFA 是一种有效的选择性 haspin 抑制剂,IC50 值为 2 nM。CHR-6494 TFA 能够抑制组蛋白 H3T3 的磷酸化。CHR-6494 TFA 诱导黑色素瘤、乳腺癌等肿瘤细胞凋亡 (apoptosis)。CHR-6494 TFA 可用于癌症的研究。

CHR-6494 TFA

CHR-6494 TFA Chemical Structure

CAS No. : 1458630-17-5

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CHR-6494 TFA 的其他形式现货产品:

CHR-6494

生物活性

CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer[1][2][3].

IC50 & Target[1]

haspin

2 nM (IC50)

体外研究
(In Vitro)

CHR-6494 (TFA; 0-105 nM; 72 hours) dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cells, with IC50s of 500 nM, 473 nM, 752 nM and 1059 nM, respectively[1].
CHR-6494 (TFA; 500 nM) produces a mitotic catastrophe with abnormal morphology of the mitotic spindle and centrosome amplification, and upregulates the spindle assembly checkpoint protein BUB1 and the marker of mitotic arrest cyclin B1[1].
CHR-6494 (TFA; 0, 0.5, 1.0 μM; 24 to 36 h) is an inhibitor of angiogenesis in the ex vivo chicken embryo aortic arch ring assay[1].
CHR-6494 (TFA) exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC50s ranging from 396 nM to 1229 nM[2].
CHR-6494 (TFA; 300 nM and 600 nM; 72 hours) induces apoptosis, increases caspase 3/7 activity by 3- and 6-fold, respectively in COLO-792 cells, and to 8.5- and 16-fold in RPMI-7951 melanoma cells[2].
CHR-6494 (TFA; 50, 200 nM; 1 week) enhances the antiproliferative effects of MLN8237 in MDA-MB-231, SKBR3 breast cancer cells[3].
CHR-6494 (TFA; 200 nM; 72 hours) enhances the apoptosis of MDA-MB-231 and SKBR3 cells when combined with MLN8237[3].

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

体内研究
(In Vivo)

CHR-6494 (TFA; 50 mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor in nude mice bearing HCT-116 human colorectal cancer cells[1].
CHR-6494 (TFA; 20 mg/kg; intraperitoneal injection for 15 consecutive days) inhibits the tumor growth in nude mice bearing MDA-MB-231 xenograft tumors[3].

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

Animal Model: Male 4-5 weeks old athymic nu/nu mice harboring HCT-116 cells xenograft tumor with a tumor volume of 200 mm3[1]
Dosage: 50 mg/kg (diluted in a solution of 10% DMSO/20% 2-hydroxypropyl-b-cyclodextrin)
Administration: i.p. in two cycles of five consecutive days for 15 days
Result: Dose-dependent tumor growth inhibition was demonstrated.
Did not change the body weight of mice.
Animal Model: 4‐week‐old female nude mice bearing MDA-MB-231 xenograft tumors
Dosage: 20 mg/kg in a final formulation in 10% DMSO/20% 2‐hydroxypropyl‐β‐cyclodextrin
Administration: i.p. for 15 consecutive days
Result: Inhibited the tumor volume and weight compared with the control group in nude mice bearing MDA-MB-231 xenograft tumors.
Enhanced the tumor volume and weight inhibition of MLN8237 (20 mg/kg; p.o.) in vivo.

分子量

406.36

Formula

C18H17F3N6O2

CAS 号

1458630-17-5

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]. Huertas D, et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene. 2012 Mar 15;31(11):1408-18.

    [2]. Han L, et al. Anti-Melanoma Activities of Haspin Inhibitor CHR-6494 Deployed as a Single Agent or in a Synergistic Combination with MEK Inhibitor. J Cancer. 2017 Aug 25;8(15):2933-2943.

    [3]. Chen A, et al. CRISPR/Cas9 screening identifies a kinetochore-microtubule dependent mechanism for Aurora-A inhibitor resistance in breast cancer. Cancer Commun (Lond). 2021 Feb;41(2):121-139.

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SHP2 protein degrader-1

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。

SHP2 protein degrader-1 

SHP2 protein degrader-1 是一种有效的 SHP2 变构抑制剂。SHP2 蛋白降解剂-1 诱导 SHP2 降解和细胞凋亡。SHP2 蛋白降解剂-1 具有研究 SHP2 相关疾病的潜力。

SHP2 protein degrader-1

SHP2 protein degrader-1 Chemical Structure

CAS No. : 2624181-69-5

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生物活性

SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases[1].

IC50 & Target

SHP2[1]

体外研究
(In Vitro)

SHP2 protein degrader-1 (compound SP4) (0-200 μM; 24 hours) inhibits the growth of Hela cells, with IC50 of 5.77 and 4.30 nM, respectively, which are about 100 times higher than the activity of SHP099 (SHP2 inhibitor)[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces 54.01% apoptotic death compared with 0.13% of the control at 100 nM[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces cell cycle arrested at the G1 phase in Hela cells[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) significantly inhibits the phosphorylation of JNK, Erk and p38[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) inhibits RAS/MAPK signaling and cellular responses by a mechanism involving inhibition of SHP2 catalytic activity[1].

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

Cell Viability Assay[1]

Cell Line: Hela cells
Concentration: 0-200  μM
Incubation Time: 24 hours
Result: Strongly inhibited the growth of Hela cells, with IC50 of 5.77 and 4.30 nM, respectively, which were about 100 times higher than the activity of SHP099 (SHP2 inhibitor).

Apoptosis Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Induced 54.01% apoptotic death compared with 0.13% of the control at 100 nM. While SHP099 at 1000 nM could induce 33.74% apoptotic death compared with 0.13% of the control.

Cell Cycle Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Induced cell cycle arrested at the G1 phase in Hela cells.

Western Blot Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Significantly inhibited the phosphorylation of JNK, Erk and p38.

分子量

908.83

Formula

C42H51Cl2N11O8

CAS 号

2624181-69-5

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]. Zheng M, et al. Novel PROTACs for degradation of SHP2 protein. Bioorg Chem. 2021;110:104788.

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UPCDC-30245

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。

UPCDC-30245 

UPCDC-30245 是一种变构 p97 (allosteric p97) 抑制剂,IC50 约为 27 nM。UPCDC-30245 抑制 p97 突变体 N660K 的效力与野生型 (IC50=300 nM) 相似,此外对 p97 突变体 T688A 仅表现出 3 倍的耐药性。UPCDC-30245可用于癌症研究。

UPCDC-30245

UPCDC-30245 Chemical Structure

CAS No. : 1883351-01-6

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生物活性

UPCDC-30245 is an allosteric p97 inhibitor with an IC50 of approximately 27 nM[1]. UPCDC-30245 inhibits the p97 mutant N660K similar to wild type (WT; IC50=300 nM) and shows 3-fold resistance for p97 mutant T688A[2]. UPCDC-30245 can be used in the research of cancer[1][2][3].

IC50 & Target[1][2]

allosteric p97

27 nM (IC50)

wild type p97

300 nM (IC50)

体外研究
(In Vitro)

UPCDC-30245 binds at the junction between the D1 dan D2 domains of p97[1].
UPCDC-30245 inhibits cell proliferation in HeLa, A549, BxPC-3, PRMI8226, MM1S, HCT116 cells, and appears more potent in HT29 cells[2].
UPCDC-30245 (0.01-100 μM) shows anti-proliferative effects on parental and CB-5083 resistant HCT116 cell lines that harbor a new p97 double mutation (D649A/T688A)[2].
UPCDC-30245 (4 μm; 2, 6, 10, 18, 24 hours; functional enrichment analysis) is not linked to pathways typically impacted by p97 inhibition, such as protein processing in the ER, UPR, and asparagine N-linked glycosylation[3].

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

分子量

463.63

Formula

C28H38FN5

CAS 号

1883351-01-6

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]. Banerjee S, et al. 2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition. Science. 2016 Feb 19;351(6275):871-5.

    [2]. Wang F, et al. Allosteric p97 Inhibitors Can Overcome Resistance to ATP-Competitive p97 Inhibitors for Potential Anticancer Therapy. ChemMedChem. 2020 Apr 20;15(8):685-694.

    [3]. Wang F, et al. Temporal proteomics reveal specific cell cycle oncoprotein downregulation by p97/VCP inhibition. Cell Chem Biol. 2021 Nov 23:S2451-9456(21)00482-7.

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MS37452

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。

MS37452  纯度: 99.22%

MS37452 是一种有效的 CBX7 chromodomain 与 H3K27me3 结合的抑制剂,Kd 为 27.7 μM。MS37452 可以通过置换 CBX7 与前列腺癌细胞中 INK4A/ARF 基因座的结合来抑制多梳抑制复合物靶基因 p16/CDKN2A 的转录。

MS37452

MS37452 Chemical Structure

CAS No. : 423748-02-1

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5 mg ¥1500 In-stock
10 mg ¥2400 In-stock
25 mg ¥4800 In-stock
50 mg ¥7650 In-stock
100 mg ¥12200 In-stock
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MS37452 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells[1].

IC50 & Target

CBX7[1]

体外研究
(In Vitro)

MS37452 (125-500 μM; 12 hours) significantly increases INK4A/ARF transcript levels up to 25% and 60% for 250 μM and 500 μM, respectively, as compared to the DMSO control[1].
MS37452 (250 μM; 2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus[1].
MS37452 (200 µM; 5 days) combined with doxorubicin results in consistently decreased cell viability compared to DMSO treated and single drug treatment[2].
MS37452 (200 µM; 5 days), which is a CBX7 chromodomain inhibitor (CBX7i), in combination with doxorubicin is a novel therapeutic strategy[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.

RT-PCR[1]

Cell Line: PC3 cells
Concentration: 125-500 μM
Incubation Time: 12 hours
Result: Up-regulated INK4A/ARF expression up to 25% and 60% for 250 μM and 500 μM, respectively.

Cell Viability Assay[2]

Cell Line: Glioblastoma multiforme (GBM) U118MG cells
Concentration: PRT4165 40 µM, PTC209 200 nM, DZnep 25 µM, GSK343 400 nM, MS37452 200 µM, Doxorubicin 200 nM, temozolomide 50 µM, SAHA 1 µM
Incubation Time: 5 days
Result: Identified several combinations that resulted in consistently decreased cell viability compared to DMSO treated and single drug treatment: SAHA/TMZ and MS37452/doxorubicin.

分子量

398.45

Formula

C22H26N2O5

CAS 号

423748-02-1

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 : 100 mg/mL (250.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5097 mL 12.5486 mL 25.0972 mL
5 mM 0.5019 mL 2.5097 mL 5.0195 mL
10 mM 0.2510 mL 1.2549 mL 2.5097 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 (6.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.27 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 (6.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.27 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
*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]. Ren C, et al. Small-molecule modulators of methyl-lysine binding for the CBX7 chromodomain. Chem Biol. 2015;22(2):161-168.

    [2]. Connelly KE, et al. CBX Chromodomain Inhibition Enhances Chemotherapy Response in Glioblastoma Multiforme. Yale J Biol Med. 2016;89(4):431-440.

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Boc-NH-PEG11-OH

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。

Boc-NH-PEG11-OH 

Boc-NH-PEG11-OH 是一种 PROTAC linker,属于 PEG 类。可用于合成 PROTAC 分子。

Boc-NH-PEG11-OH

Boc-NH-PEG11-OH Chemical Structure

CAS No. : 1556847-53-0

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生物活性

Boc-NH-PEG11-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

分子量

601.72

Formula

C27H55NO13

CAS 号

1556847-53-0

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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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MIF-IN-5

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。

MIF-IN-5 

MIF-IN-5 (compound 1d) 是一种有效、可逆的巨噬细胞迁移抑制因子 (MIF) 竞争性抑制剂,IC50 为 4.8 μM,Ki 为 3.3 μM。

MIF-IN-5

MIF-IN-5 Chemical Structure

CAS No. : 2582755-31-3

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生物活性

MIF-IN-5 (compound 1d) is a potent and reversible macrophage migration inhibitory factor (MIF) competitive inhibitor with an IC50 of 4.8 μM and a Ki value of 3.3 μM, respectively[1].

IC50 & Target

IC50: 4.8 μM (MIF)[1]
Ki: 3.3 μM (MIF)[1]

分子量

351.33

Formula

C18H14FN5O2

CAS 号

2582755-31-3

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]. Xiao Z, Fokkens M, Chen D, et al. Structure-activity relationships for binding of 4-substituted triazole-phenols to macrophage migration inhibitory factor (MIF). Eur J Med Chem. 2020;186:111849.

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CGP-82996(Synonyms: CINK4)

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。

CGP-82996 (Synonyms: CINK4)

GP-82996 (CINK4) 是 CDK4/6 的药理学抑制剂。GP-82996 对 CDK4/cyclin D1、CDK6/cyclin D1 和 Cdk5/p35 的 IC50s 分别为 1.5、5.6 和 25 μM。GP-82996 诱导肿瘤细胞 U2OS 的凋亡 (apoptosis)。GP-82996可用于癌症研究。

CGP-82996(Synonyms: CINK4)

CGP-82996 Chemical Structure

CAS No. : 359886-84-3

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生物活性

GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer[1][2].

IC50 & Target[1]

Cdk4/cyclin D1

1.5 μM (IC50)

CDK6/cyclinD1

5.6 μM (IC50)

CDK5/p35

25 μM (IC50)

CDK2/cyclinA

>50 μM (IC50)

CDK1/cyclinB

>100 μM (IC50)

CDK2/cyclin E

>50 μM (IC50)

CDK4/cyclin D2

>50 μM (IC50)

Cdk6/cyclin D2

>50 μM (IC50)

V-abl

>10 μM (IC50)

c-met

>10 μM (IC50)

IGF-1R

>10 μM (IC50)

Insulin-R

>10 μM (IC50)

体外研究
(In Vitro)

GP-82996 (5, 10 μM; 24 hours) induces G1 arrest and G0-G1/S ratio increase in U2OS (p16 negative) and MRC-5 (p16 positive) cells[1].
GP-82996 (5, 10 μM; 24 hours) reduces hyperphosphorylation of pRb, but has no changes in the levels of CDK4 in U2OS, MRC-5 cells[1].
GP-82996 (5, 10 μM; 48 hours) induces aooptosis in 83% of U2OS cells in concentration of 10μM[1].
GP-82996 (0.1-40 μM; 24,48, 72 hours) inhibits the cell proliferation of A549, H358, SKLU-1, H23, PC14 cells with IC50 values of 72 h are 4-7 μM[2].
GP-82996 (3, 5, 10 μM; 48 hours) induces G1 arrest in A549 and H23 cells[2].
GP-82996 ((1, 3, 5, 10 μM; 72 hours) enhances Paclitaxel sensitivity in KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23 cells) [2].
GP-82996 (10 μM; 72 hours) combined with Paclitaxel (3 nM; 72 hours) increases the apoptosis of A549 and H23 cells[2].

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

体内研究
(In Vivo)

GP-82996 (30 mg/kg, i.p. for 29 days) shows smaller final tumor volume compared with vehicle control in mouse xenograft models[1].

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

Animal Model: 19-21 g female BALB/c nu/nu mice xenograft model (HCT116 tumors volume=100 mm3)[1]
Dosage: 30 mg/kg
Administration: i.p. every 12 hours for 29 days
Result: Showed smaller final tumor volume compared with vehicle control in mouse xenograft models.

分子量

456.58

Formula

C27H32N6O

CAS 号

359886-84-3

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.

溶解性数据
In Vivo:
  • 1.

    5% DMSO, 0.05% Tween 80, and 95% physiologic saline

参考文献
  • [1]. Soni R, et al. Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4. J Natl Cancer Inst. 2001 Mar 21;93(6):436-46.

    [2]. Zhang XH, et al. A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS. Cancer Biol Ther. 2013;14(7):597-605.

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CHR-6494 TFA

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。

CHR-6494 TFA 

CHR-6494 TFA 是一种有效的选择性 haspin 抑制剂,IC50 值为 2 nM。CHR-6494 TFA 能够抑制组蛋白 H3T3 的磷酸化。CHR-6494 TFA 诱导黑色素瘤、乳腺癌等肿瘤细胞凋亡 (apoptosis)。CHR-6494 TFA 可用于癌症的研究。

CHR-6494 TFA

CHR-6494 TFA Chemical Structure

CAS No. : 1458630-17-5

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CHR-6494 TFA 的其他形式现货产品:

CHR-6494

生物活性

CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer[1][2][3].

IC50 & Target[1]

haspin

2 nM (IC50)

体外研究
(In Vitro)

CHR-6494 (TFA; 0-105 nM; 72 hours) dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cells, with IC50s of 500 nM, 473 nM, 752 nM and 1059 nM, respectively[1].
CHR-6494 (TFA; 500 nM) produces a mitotic catastrophe with abnormal morphology of the mitotic spindle and centrosome amplification, and upregulates the spindle assembly checkpoint protein BUB1 and the marker of mitotic arrest cyclin B1[1].
CHR-6494 (TFA; 0, 0.5, 1.0 μM; 24 to 36 h) is an inhibitor of angiogenesis in the ex vivo chicken embryo aortic arch ring assay[1].
CHR-6494 (TFA) exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC50s ranging from 396 nM to 1229 nM[2].
CHR-6494 (TFA; 300 nM and 600 nM; 72 hours) induces apoptosis, increases caspase 3/7 activity by 3- and 6-fold, respectively in COLO-792 cells, and to 8.5- and 16-fold in RPMI-7951 melanoma cells[2].
CHR-6494 (TFA; 50, 200 nM; 1 week) enhances the antiproliferative effects of MLN8237 in MDA-MB-231, SKBR3 breast cancer cells[3].
CHR-6494 (TFA; 200 nM; 72 hours) enhances the apoptosis of MDA-MB-231 and SKBR3 cells when combined with MLN8237[3].

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

体内研究
(In Vivo)

CHR-6494 (TFA; 50 mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor in nude mice bearing HCT-116 human colorectal cancer cells[1].
CHR-6494 (TFA; 20 mg/kg; intraperitoneal injection for 15 consecutive days) inhibits the tumor growth in nude mice bearing MDA-MB-231 xenograft tumors[3].

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

Animal Model: Male 4-5 weeks old athymic nu/nu mice harboring HCT-116 cells xenograft tumor with a tumor volume of 200 mm3[1]
Dosage: 50 mg/kg (diluted in a solution of 10% DMSO/20% 2-hydroxypropyl-b-cyclodextrin)
Administration: i.p. in two cycles of five consecutive days for 15 days
Result: Dose-dependent tumor growth inhibition was demonstrated.
Did not change the body weight of mice.
Animal Model: 4‐week‐old female nude mice bearing MDA-MB-231 xenograft tumors
Dosage: 20 mg/kg in a final formulation in 10% DMSO/20% 2‐hydroxypropyl‐β‐cyclodextrin
Administration: i.p. for 15 consecutive days
Result: Inhibited the tumor volume and weight compared with the control group in nude mice bearing MDA-MB-231 xenograft tumors.
Enhanced the tumor volume and weight inhibition of MLN8237 (20 mg/kg; p.o.) in vivo.

分子量

406.36

Formula

C18H17F3N6O2

CAS 号

1458630-17-5

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]. Huertas D, et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene. 2012 Mar 15;31(11):1408-18.

    [2]. Han L, et al. Anti-Melanoma Activities of Haspin Inhibitor CHR-6494 Deployed as a Single Agent or in a Synergistic Combination with MEK Inhibitor. J Cancer. 2017 Aug 25;8(15):2933-2943.

    [3]. Chen A, et al. CRISPR/Cas9 screening identifies a kinetochore-microtubule dependent mechanism for Aurora-A inhibitor resistance in breast cancer. Cancer Commun (Lond). 2021 Feb;41(2):121-139.

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Verrucarin J(Synonyms: Muconomycin B)

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。

Verrucarin J (Synonyms: Muconomycin B)

Verrucarin J (Muconomycin B) 是 Myrothecium 真菌家族的代谢物。Verrucarin J 诱导活性氧 (ROS) 生成和癌细胞系凋亡 (apoptosis),例如 A549、HCT 116 和 SW-620 细胞。Verrucarin J 具有抗 Candida albicansMucor miehei 的活性。Verrucarin J 抑制沙粒病毒 Junin (JUNV) 产量,IC50 为 1.2 ng/mL。

Verrucarin J(Synonyms: Muconomycin B)

Verrucarin J Chemical Structure

CAS No. : 4643-58-7

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生物活性

Verrucarin J (Muconomycin B) is a metabolite of the Myrothecium fungus family. Verrucarin J generates reactive oxygen species (ROS) and induces apoptosis of cancer cell lines, such as A549, HCT 116 and SW-620 cells. Verrucarin J shows activities against Candida albicans and Mucor miehei. Verrucarin J inhibits arenavirus Junin (JUNV) yield with an IC50 of 1.2 ng/mL[1][2][3][4][5].

体外研究
(In Vitro)

Verrucarin J (0, 5, 10, 20, 50 nM; 24 hours) induces the apoptosis of A549 cells[1].
Verrucarin J (0, 1, 2, 5, 10, 20, 50 nM; 24, 48, 72 hours) significantly inhibits cell proliferation of A549 and H1793 cells with IC50 values of approximately 10 nM and 20 nM after 48 h of treatment, respectively[1].
Verrucarin J (0, 0.1, 0.2, 0.3, 0.4, 0.5 μM; 24 hours) has an IC50 of 300 nM for HCT 116 and SW-620 cell proliferation[2].
Verrucarin J (0, 10, 20 nM, 48 hours) inhibits cancer stem cell (CSC) self-renewal pathways Wnt1/β-catenin and Notch1 and down-regulates the expression of key CSC specific genes (ALDH1, LGR5, OCT4 and CD133) of A549 cells[1].
Verrucarin J (compound 2; 50 μg/disk) shows noteworthy activities against Candida albicans and Mucor miehei[3].
Verrucarin J reduces JUNV yield more than 2 log units and has a similar effect against the arenavirus Tacaribe[4].
Verrucarin J reduces the cell viability of Vero cells with a cytotoxic concentration 50% (CC50) of 8.2 ng/mL[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.

体内研究
(In Vivo)

Verrucarin J (0.5 mg/kg; i.p. for 4 weeks) suppresses AKT-induced tumor growth in a xenograft model[2].
Verrucarin J (0.1, 0.5, 2.0 mg/kg; i.p. for three weeks) is a highly potent anticancer drug and suppresses tumor growth and metastasis[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.

Animal Model: 6-8 weeks old BALB/c athymic nude mice (nu/nu) with pCMV/HCT 116 and AKT/HCT 116 xenografts[2]
Dosage: 0.5 mg/kg body weight
Administration: i.p. for 4 weeks
Result: Reduced the expression of prosurvival markers pAKT, Notch1, p65, and Ki67 in all tumors.
Animal Model: Female nude nu/nu (5 to 6 weeks old) mice with A2780 xenografts[5]
Dosage: 0.1, 0.5, 2.0 mg/kg (vehicle: 10% DMSO, 90% glyceryl trioctanoate)
Administration: i.p. for three weeks after 10 days of injection of A2780 cells
Result: Reduced tumor weight (32% lower compared to control), and reduced visible metastasis in 0.1 mg/kg.
Showed a significant reduction in visible peritoneal tumors (61% lower compared to control group) and highly reduced visible metastasis in 0.5 mg/kg.
Reduced ovarian tumor weight by 71% compared to vehicle in 0.5 mg/kg.
In lethal dose 2 mg/kg, mice sick with a swollen belly, body fluid and subsequently died within 3 treatments.

分子量

484.54

Formula

C27H32O8

CAS 号

4643-58-7

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]. Udoh K, et al. Targeting of Lung Cancer Stem Cell Self-Renewal Pathway by a Small Molecule Verrucarin J. Stem Cell Rev Rep. 2019 Aug;15(4):601-611.

    [2]. Pal D, et al. Suppression of Notch1 and AKT mediated epithelial to mesenchymal transition by Verrucarin J in metastatic colon cancer. Cell Death Dis. 2018 Jul 23;9(8):798.

    [3]. Mondol MA, et al. Macrocyclic Trichothecenes from Myrothecium roridum Strain M10 with Motility Inhibitory and Zoosporicidal Activities against Phytophthora nicotianae. J Agric Food Chem. 2015 Oct 14;63(40):8777-86.

    [4]. García CC, et al, Damonte EB. Evaluation of the antiviral activity against Junin virus of macrocyclic trichothecenes produced by the hypocrealean epibiont of Baccharis coridifolia. Planta Med. 2002 Mar;68(3):209-12.

    [5]. Carter K, et al. Verrucarin J inhibits ovarian cancer and targets cancer stem cells. Oncotarget. 2017 Oct 6;8(54):92743-92756.

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GSA-10

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。

GSA-10 

GSA-10 是一种有效的平滑 (Smo) 受体激动剂,其 EC50 值为 1.2 μM。GSA-10 是一种新型喹啉甲酰胺衍生物。GSA-10 作用于 Smo,促进多能间充质干细胞分化为成骨细胞。GSA-10 介导 Hedgehog (Hh) 信号传导,这可能对癌症疾病的再生医学具有研究意义。

GSA-10

GSA-10 Chemical Structure

CAS No. : 300833-95-8

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生物活性

GSA-10 is a potent agonist of Smoothened (Smo) receptor with an EC50 of 1.2 μM. GSA-10 is a novel quinolinecarboxamide derivative. GSA-10 acts at Smo to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts. GSA-10 mediates Hedgehog (Hh) signaling which may have researching interests in regenerative medicine for cancer disease[1][2].

IC50 & Target

Smoothened receptor[1]

分子量

450.53

Formula

C26H30N2O5

CAS 号

300833-95-8

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]. Manetti F, et al. Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives. Eur J Med Chem. 2016;121:747-757.

    [2]. Gorojankina T, et al. Discovery, molecular and pharmacological characterization of GSA-10, a novel small-molecule positive modulator of Smoothened [published correction appears in Mol Pharmacol. 2013 Aug;84(2):303]. Mol Pharmacol. 2013;83(5):1020-1029.

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TNIK-IN-2

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。

TNIK-IN-2 

TNIK-IN-2 是一种 TNIK 抑制剂,IC50 值为 1.3337 μM。

TNIK-IN-2

TNIK-IN-2 Chemical Structure

CAS No. : 2754265-76-2

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生物活性

TNIK-IN-2 is a Traf2- and Nck-interacting protein kinase (TNIK) inhibitor, with an IC50 of 1.3337 μM[1].

IC50 & Target

IC50: 1.3337 μM (TNIK)[1]

体外研究
(In Vitro)

TNIK-IN-2 (compound 1) inhibits TNIK, with an IC50 of 31.26 μM in HCT116 cells[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

373.40

Formula

C22H19N3O3

CAS 号

2754265-76-2

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]. Li Y, et, al. Discovery of 3,4-Dihydrobenzo[ f][1,4]oxazepin-5(2 H)-one Derivatives as a New Class of Selective TNIK Inhibitors and Evaluation of Their Anti-Colorectal Cancer Effects. J Med Chem. 2022 Jan 5.

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UPCDC-30245

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。

UPCDC-30245 

UPCDC-30245 是一种变构 p97 (allosteric p97) 抑制剂,IC50 约为 27 nM。UPCDC-30245 抑制 p97 突变体 N660K 的效力与野生型 (IC50=300 nM) 相似,此外对 p97 突变体 T688A 仅表现出 3 倍的耐药性。UPCDC-30245可用于癌症研究。

UPCDC-30245

UPCDC-30245 Chemical Structure

CAS No. : 1883351-01-6

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生物活性

UPCDC-30245 is an allosteric p97 inhibitor with an IC50 of approximately 27 nM[1]. UPCDC-30245 inhibits the p97 mutant N660K similar to wild type (WT; IC50=300 nM) and shows 3-fold resistance for p97 mutant T688A[2]. UPCDC-30245 can be used in the research of cancer[1][2][3].

IC50 & Target[1][2]

allosteric p97

27 nM (IC50)

wild type p97

300 nM (IC50)

体外研究
(In Vitro)

UPCDC-30245 binds at the junction between the D1 dan D2 domains of p97[1].
UPCDC-30245 inhibits cell proliferation in HeLa, A549, BxPC-3, PRMI8226, MM1S, HCT116 cells, and appears more potent in HT29 cells[2].
UPCDC-30245 (0.01-100 μM) shows anti-proliferative effects on parental and CB-5083 resistant HCT116 cell lines that harbor a new p97 double mutation (D649A/T688A)[2].
UPCDC-30245 (4 μm; 2, 6, 10, 18, 24 hours; functional enrichment analysis) is not linked to pathways typically impacted by p97 inhibition, such as protein processing in the ER, UPR, and asparagine N-linked glycosylation[3].

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

分子量

463.63

Formula

C28H38FN5

CAS 号

1883351-01-6

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]. Banerjee S, et al. 2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition. Science. 2016 Feb 19;351(6275):871-5.

    [2]. Wang F, et al. Allosteric p97 Inhibitors Can Overcome Resistance to ATP-Competitive p97 Inhibitors for Potential Anticancer Therapy. ChemMedChem. 2020 Apr 20;15(8):685-694.

    [3]. Wang F, et al. Temporal proteomics reveal specific cell cycle oncoprotein downregulation by p97/VCP inhibition. Cell Chem Biol. 2021 Nov 23:S2451-9456(21)00482-7.

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MRT-83 hydrochloride

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。

MRT-83 hydrochloride  纯度: 99.60%

MRT-83 (hydrochloride) 是 Smoothened (Smo) 受体的有效拮抗剂。MRT-83 (hydrochloride) 抑制 Hedgehog (Hh) 信号通路和 BODIPY-cyclopamine 与人 Smo 的结合。MRT-83 (hydrochloride) 具有研究癌症疾病的潜力。

MRT-83 hydrochloride

MRT-83 hydrochloride Chemical Structure

CAS No. : 1359944-60-7

规格 价格 是否有货 数量
5 mg ¥1200 In-stock
10 mg ¥1900 In-stock
25 mg ¥3900 In-stock
50 mg ¥6700 In-stock
100 mg ¥11500 In-stock
200 mg   询价  
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MRT-83 hydrochloride 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

MRT-83 (hydrochloride) is the potent antagonist of Smoothened (Smo) receptor. MRT-83 (hydrochloride) inhibits the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo. MRT-83 (hydrochloride) has the potential for researching cancer disease[1].

IC50 & Target

Smo[1]

体外研究
(In Vitro)

MRT-83 (hydrochloride) (compound 86) has IC50s of 15 and 11 nM respectively in Shh-light2 and C3H10T1/2 cells in the biological activity assay[1].

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

分子量

575.05

Formula

C31H31ClN4O5

CAS 号

1359944-60-7

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 : 250 mg/mL (434.74 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7390 mL 8.6949 mL 17.3898 mL
5 mM 0.3478 mL 1.7390 mL 3.4780 mL
10 mM 0.1739 mL 0.8695 mL 1.7390 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。

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 (3.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.62 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 (3.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.62 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
  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.62 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 20.8 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Solinas A, et al. Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity. J Med Chem. 2012;55(4):1559-1571.

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Ajoene

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。

Ajoene 

Ajoene 是一种大蒜衍生化合物,是一种抗血栓和抗真菌剂。Ajoene 抑制HL-60、U937、HEL 和 OCIM-I 等白血病 CD34 阴性细胞的增殖并诱导其凋亡。具有抗癌活性。

Ajoene

Ajoene Chemical Structure

CAS No. : 92285-01-3

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

Ajoene, a garlic-derived compound, is an antithrombotic and antifungal agent. Ajoene inhibits proliferation and induces apoptosis of human leukaemia CD34-negative cells including HL-60, U937, HEL and OCIM-I. Anticancer activities[1][2].

体外研究
(In Vitro)

Ajoene shows cytotoxicity with IC50s in the 7-41 uM range for B16/BL6, HT-29, A549, MDA-MB231, PANC-1, and SKBR-3 cells[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)

Ajoene (25 μg/g body weight of Ajoene in 100 mL Intralipid; i.p.; every other day from the day of inoculation up to day 28) inhibits both primary tumor growth[1].
Ajoene (25, 15 or 5 μg/g body weight of Ajoene in 100 μL Intralipid; i.p; every other day over 4 weeks) inhibits strongly metastasis to lung in the B16/BL6 melanoma tumor model in C57BL/6 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.

分子量

234.40

Formula

C9H14OS3

CAS 号

92285-01-3

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]. Taylor P, et al. Ajoene inhibits both primary tumor growth and metastasis of B16/BL6 melanoma cells in C57BL/6 mice. Cancer Lett. 2006;239(2):298-304.

    [2]. Ahmed N, et al. Ajoene, a garlic-derived natural compound, enhances chemotherapy-induced apoptosis in human myeloid leukaemia CD34-positive resistant cells. Anticancer Res. 2001;21(5):3519-3523.

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CGP-82996(Synonyms: CINK4)

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。

CGP-82996 (Synonyms: CINK4)

GP-82996 (CINK4) 是 CDK4/6 的药理学抑制剂。GP-82996 对 CDK4/cyclin D1、CDK6/cyclin D1 和 Cdk5/p35 的 IC50s 分别为 1.5、5.6 和 25 μM。GP-82996 诱导肿瘤细胞 U2OS 的凋亡 (apoptosis)。GP-82996可用于癌症研究。

CGP-82996(Synonyms: CINK4)

CGP-82996 Chemical Structure

CAS No. : 359886-84-3

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

GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer[1][2].

IC50 & Target[1]

Cdk4/cyclin D1

1.5 μM (IC50)

CDK6/cyclinD1

5.6 μM (IC50)

CDK5/p35

25 μM (IC50)

CDK2/cyclinA

>50 μM (IC50)

CDK1/cyclinB

>100 μM (IC50)

CDK2/cyclin E

>50 μM (IC50)

CDK4/cyclin D2

>50 μM (IC50)

Cdk6/cyclin D2

>50 μM (IC50)

V-abl

>10 μM (IC50)

c-met

>10 μM (IC50)

IGF-1R

>10 μM (IC50)

Insulin-R

>10 μM (IC50)

体外研究
(In Vitro)

GP-82996 (5, 10 μM; 24 hours) induces G1 arrest and G0-G1/S ratio increase in U2OS (p16 negative) and MRC-5 (p16 positive) cells[1].
GP-82996 (5, 10 μM; 24 hours) reduces hyperphosphorylation of pRb, but has no changes in the levels of CDK4 in U2OS, MRC-5 cells[1].
GP-82996 (5, 10 μM; 48 hours) induces aooptosis in 83% of U2OS cells in concentration of 10μM[1].
GP-82996 (0.1-40 μM; 24,48, 72 hours) inhibits the cell proliferation of A549, H358, SKLU-1, H23, PC14 cells with IC50 values of 72 h are 4-7 μM[2].
GP-82996 (3, 5, 10 μM; 48 hours) induces G1 arrest in A549 and H23 cells[2].
GP-82996 ((1, 3, 5, 10 μM; 72 hours) enhances Paclitaxel sensitivity in KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23 cells) [2].
GP-82996 (10 μM; 72 hours) combined with Paclitaxel (3 nM; 72 hours) increases the apoptosis of A549 and H23 cells[2].

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

体内研究
(In Vivo)

GP-82996 (30 mg/kg, i.p. for 29 days) shows smaller final tumor volume compared with vehicle control in mouse xenograft models[1].

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

Animal Model: 19-21 g female BALB/c nu/nu mice xenograft model (HCT116 tumors volume=100 mm3)[1]
Dosage: 30 mg/kg
Administration: i.p. every 12 hours for 29 days
Result: Showed smaller final tumor volume compared with vehicle control in mouse xenograft models.

分子量

456.58

Formula

C27H32N6O

CAS 号

359886-84-3

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.

溶解性数据
In Vivo:
  • 1.

    5% DMSO, 0.05% Tween 80, and 95% physiologic saline

参考文献
  • [1]. Soni R, et al. Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4. J Natl Cancer Inst. 2001 Mar 21;93(6):436-46.

    [2]. Zhang XH, et al. A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS. Cancer Biol Ther. 2013;14(7):597-605.

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Palmitic acid-13C 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。

Palmitic acid-13C sodium 

Palmitic acid-13C sodium 是一种 13C 标记的 Palmitic acid sodium。Palmitic acid sodium 一种常见于动物和植物中的长链饱和脂肪酸。Palmitic acid sodium 以诱导小鼠颗粒细胞中葡萄糖调节蛋白 78 (GRP78) 和 CCAAT/增强子结合蛋白同源蛋白 (CHOP) 的表达。

Palmitic acid-13C sodium

Palmitic acid-13C sodium Chemical Structure

CAS No. : 201612-54-6

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

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生物活性

Palmitic acid-13C sodium is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].

分子量

279.40

Formula

C1513CH31NaO2

CAS 号

201612-54-6

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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Harada H, et al. Antitumor activity of palmitic acid found as a selective cytotoxic substance in a marine red alga. Anticancer Res. 2002 Sep-Oct;22(5):2587-90.

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MIF-IN-6

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。

MIF-IN-6 

MIF-IN-6 (compound 2d) 是一种有效的巨噬细胞迁移抑制因子 (MIF) 抑制剂,IC50 为 1.4 μM,Ki 为 0.96 μM。MIF-IN-6 减弱 MIF 诱导的 ERK 磷酸化,抑制 A549 细胞增殖。

MIF-IN-6

MIF-IN-6 Chemical Structure

CAS No. : 2582758-61-8

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

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生物活性

MIF-IN-6 (compound 2d) is a potent macrophage migration inhibitory factor (MIF) inhibitor with an IC50 of 1.4 μM and a Ki value of 0.96 μM, respectively. MIF-IN-6 attenuates MIF-induced ERK phosphorylation and inhibits proliferation of A549 cells[1].

IC50 & Target

IC50: 1.4 μM (MIF)[1]
Ki: 0.96 μM (MIF)[1]

分子量

385.78

Formula

C18H13ClFN5O2

CAS 号

2582758-61-8

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]. Xiao Z, Fokkens M, Chen D, et al. Structure-activity relationships for binding of 4-substituted triazole-phenols to macrophage migration inhibitory factor (MIF). Eur J Med Chem. 2020;186:111849.

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Naphthofluorescein(Synonyms: Naphthafluorescein)

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。

Naphthofluorescein (Synonyms: Naphthafluorescein)

Naphthofluorescein 抑制 HIF-1 和 Mint3 之间的相互作用。Naphthofluorescein 抑制 Mint3 依赖性 HIF-1 活性以及癌细胞和巨噬细胞的糖酵解活动,同时不引起体外细胞毒性和体内副作用。Naphthofluorescein 也是一种荧光 pH 敏感探针,可用于功能性切伦科夫成像。

Naphthofluorescein(Synonyms: Naphthafluorescein)

Naphthofluorescein Chemical Structure

CAS No. : 61419-02-1

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

Naphthofluorescein inhibits the interaction between HIF-1 and Mint3. Naphthofluorescein suppresses Mint3-dependent HIF-1 activity and glycolysis in cancer cells and macrophages without cytotoxicity in vitro and adverse effect in vivo[1]. Naphthofluorescein is also a fluorescent pH-sensitive probe that can be used for functional Cerenkov imaging[2].

IC50 & Target

HIF-1[1]

体外研究
(In Vitro)

Naphthofluorescein (compound 19) (0-10 μM; 24 hours) suppresses the HIF-1 reporter activity in a concentration-dependent manner[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 Viability Assay[1]

Cell Line: HT1080 cells
Concentration: 0-10 μM
Incubation Time: 24 hours
Result: Significantly suppressed the HIF-1 reporter activity in a concentration-dependent manner.

体内研究
(In Vivo)

Naphthofluorescein (compound 19) (100 mg/kg; i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks)does not show weight loss or apparent histological abnormalities in the lung, liver, and kidney, or cause cause severe adverse effects for at least 2 weeks in mice[1].
Naphthofluorescein (compound 19) (100 mg/kg; i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks) strikingly suppresses the tumour growth of subcutaneously injected E0771 cells and significantly attenuates tumour growth of MDA-MB-231 and AsPC-1 cells in immunodeficient mice. In turn, naphthofluorescein does not attenuate tumour growth of FIH-1-depleted MDA-MB-231 cells[1].
Naphthofluorescein (compound 19) (100 mg/kg; i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks) suppresses tumour growth in human cancer cells in an FIH-1-dependent manner[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 C57BL/6J mice (8 weeks)[1]
Dosage: 100 mg/kg
Administration: i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks
Result: Neither showed weight loss or apparent histological abnormalities in the lung, liver, and kidney, or caused cause severe adverse effects for at least 2 weeks in mice.
Animal Model: Female C57BL/6J mice (E0771) and BALB/c nude mice (HT1080, MDA-MB-231, and AsPC-1) (6 weeks)[1]
Dosage: 100 mg/kg
Administration: i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks
Result: Strikingly suppressed the tumour growth of subcutaneously injected E0771 cells and significantly attenuated tumour growth of MDA-MB-231 and AsPC-1 cells in immunodeficient mice. In turn, naphthofluorescein did not attenuate tumour growth of FIH-1-depleted MDA-MB-231 cells.

分子量

432.42

Formula

C28H16O5

CAS 号

61419-02-1

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]. Sakamoto T, et al. Pharmacological inhibition of Mint3 attenuates tumour growth, metastasis, and endotoxic shock. Commun Biol. 2021;4(1):1165. Published 2021 Oct 7.

    [2]. Arroyo AD, et al. Development of fluorinated naphthofluoresceins for Cerenkov imaging. J Fluor Chem. 2019;225:27-34.

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