日度归档：2022年6月3日

NCT02

发表于由

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。

NCT02 

NCT02 是一种细胞周期蛋白 K 降解剂。NCT02 诱导细胞周期蛋白 K (CCNK) 的泛素化和 CCNK 及其复合物 CDK12 的蛋白酶体降解。NCT02具有研究转移性结直肠癌 (CRC) 的潜力。

NCT02

NCT02 Chemical Structure

CAS No. : 790245-61-3

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生物活性

NCT02 is a cyclin K degrader. NCT02 induces ubiquitination of cyclin K (CCNK) and proteasomal degradation of CCNK and its complex partner CDK12. NCT02 has the potential for the research of metastatic colorectal cancer (CRC)[1].

分子量

312.39

Formula

C17H16N2O2S
CAS 号

790245-61-3
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]. Dieter SM, et al. Degradation of CCNK/CDK12 is a druggable vulnerability of colorectal cancer. Cell Rep. 2021;36(3):109394.

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hGGPPS-IN-3

发表于由

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。

hGGPPS-IN-3 

hGGPPS-IN-3 (Compound 13h) 是人类香叶基香叶基焦磷酸合成酶 (hGGPPS) 的有效抑制剂。hGGPPS-IN-3 是 C-2 取代的噻吩并嘧啶基双膦酸盐 (C2-ThP-BPs) 的类似物。hGGPPS-IN-3 可诱导多发性骨髓瘤 (MM) 细胞的靶向选择性凋亡 (apoptosis)，并在体内表现出抗骨髓瘤活性。

hGGPPS-IN-3

hGGPPS-IN-3 Chemical Structure

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生物活性

hGGPPS-IN-3 (Compound 13h) is a potent inhibitor of the human geranylgeranyl pyrophosphate synthase (hGGPPS). hGGPPS-IN-3 is an analogue of C-2-substituted thienopyrimidine-based bisphosphonates (C2-ThP-BPs). hGGPPS-IN-3 induces target-selective apoptosis of multiple myeloma (MM) cells and exhibits antimyeloma activity in vivo[1].

分子量

613.31

Formula

C21H19BrN4O7P2S
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]. Lee HF, et al. Synthesis and Evaluation of Structurally Diverse C-2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase. J Med Chem. 2022;65(3):2471-2496.

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SB-429201

发表于由

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。

SB-429201 

SB-429201 是一种有效的选择性 HDAC1 (IC50~1.5 μM)。SB-429201 对 HDAC1 抑制的偏好至少是 HDAC3 和 HDAC8 的 20 倍。

SB-429201

SB-429201 Chemical Structure

CAS No. : 1027971-34-1

规格 价格 是否有货 数量
5 mg ￥4200 In-stock
10 mg ￥6700 In-stock
25 mg ￥13500 In-stock
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SB-429201 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

SB-429201 is a potent and selective HDAC1 (IC50~1.5 μM). SB-429201 displays at least a 20-fold preference for HDAC1 inhibition over HDAC3 and HDAC8[1][2].

IC50 & Target[1]

HDAC3

1.5 μM (IC50)

分子量

436.50

Formula

C28H24N2O3
CAS 号

1027971-34-1
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
参考文献

  • [1]. Hu E, et al. Identification of novel isoform-selective inhibitors within class I histone deacetylases. J Pharmacol Exp Ther. 2003;307(2):720-728.

    [2]. Bieliauskas AV, Pflum MK. Isoform-selective histone deacetylase inhibitors. Chem Soc Rev. 2008;37(7):1402-1413.

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ZL-Pin13

发表于由

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。

ZL-Pin13 

ZL-Pin13 是一种高效细胞活性共价抑制剂，靶向 Pin1，IC50 为 67 nM。ZL-Pin13 有效抑制 MDA-MB-231 细胞的增殖并下调 Pin1 底物。

ZL-Pin13

ZL-Pin13 Chemical Structure

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生物活性

ZL-Pin13 is a high potent cell-active covalent inhibitor targeting the Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) with an IC50 of 67 nM. ZL-Pin13 effectively inhibits the proliferation and downregulated the Pin1 substrates in MDA-MB-231 cells[1].

分子量

454.97

Formula

C24H23ClN2O3S
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]. Liu L, et al. Computational and Structure-Based Development of High Potent Cell-Active Covalent Inhibitor Targeting the Peptidyl-Prolyl Isomerase NIMA-Interacting-1 (Pin1). J Med Chem. 2022;65(3):2174-2190.

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hGGPPS-IN-1

发表于由

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。

hGGPPS-IN-1 

hGGPPS-IN-1 (Compound 18b) 是人类香叶基香叶基焦磷酸合成酶 (hGGPPS) 的有效抑制剂。hGGPPS-IN-1 是 C-2 取代的噻吩并嘧啶基双膦酸盐 (C2-ThP-BPs) 的类似物。hGGPPS-IN-1 可诱导多发性骨髓瘤 (MM) 细胞的靶向选择性凋亡 (apoptosis)，并在体内表现出抗骨髓瘤活性

hGGPPS-IN-1

hGGPPS-IN-1 Chemical Structure

CAS No. : 1429012-38-3

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生物活性

hGGPPS-IN-1 (Compound 18b) is a potent inhibitor of the human geranylgeranyl pyrophosphate synthase (hGGPPS). hGGPPS-IN-1 is an analogue of C-2-substituted thienopyrimidine-based bisphosphonates (C2-ThP-BPs). hGGPPS-IN-1 induces target-selective apoptosis of multiple myeloma (MM) cells and exhibits antimyeloma activity in vivo[1].

分子量

401.27

Formula

C13H13N3O6P2S
CAS 号

1429012-38-3
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]. Lee HF, et al. Synthesis and Evaluation of Structurally Diverse C-2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase. J Med Chem. 2022;65(3):2471-2496.

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Proteasome-IN-4

发表于由

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。

Proteasome-IN-4 

Proteasome-IN-4 是一种良好的非共价 proteasome 抑制剂 (IC50= 8.39 nM)。Proteasome-IN-4 对 RPMI-8226、MM-1S 和 MV-4-11 细胞系具有较强的抗增殖活性。Proteasome-IN-4 可用于癌症研究。

Proteasome-IN-4

Proteasome-IN-4 Chemical Structure

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生物活性

Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research[1].

IC50 & Target

IC50: 8.39 nM (proteasome)[1]
体外研究
(In Vitro)

Proteasome-IN-4 (compound 43) (0-20 nM; 72 hours) has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively[1].
Proteasome-IN-4 (10-1000 nM; 3 hours) causes massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM[1].
Proteasome-IN-4 (2μM) has high metabolic stability in mouse blood, with T1/2 of 329.21 min[1].

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

Cell Proliferation Assay

Cell Line: MM-1S, RPMI 8226 and MV-4-11 cells[1]
Concentration: 0-20 nM
Incubation Time: 72 hours
Result: Displayed potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively.

Western Blot Analysis

Cell Line: MM-1S[1]
Concentration: 10, 100 and 1000 nM
Incubation Time: 3 hours
Result: Caused massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM.

体内研究
(In Vivo)

Proteasome-IN-4 (5 mg/kg; i.v.; single) has superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h in model mice[1].

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

Animal Model: ICR mice (6-8 weeks)[1]
Dosage: 5 mg/kg
Administration: i.v.; single
Result: Displayed superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h.

分子量

750.97

Formula

C44H58N6O5
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]. Cao Y, et al. Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment. Eur J Med Chem. 2022;233:114211.

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LSD1-IN-14

发表于由

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。

LSD1-IN-14 

LSD1-IN-14 是一种有效且具有选择性的 LSD1 抑制剂 (IC50=0.89 μM)。LSD1-IN-14 能显著抑制 A549 和 THP-1 细胞的增殖，能诱导肿瘤细胞的凋亡。

LSD1-IN-14

LSD1-IN-14 Chemical Structure

CAS No. : 2698340-11-1

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生物活性

LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells[1].

IC50 & Target

IC50: 0.89 μM (LSD1)[1]
体外研究
(In Vitro)

LSD1-IN-14 (compound x43) (0-20 μM; 72 hours) has a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively[1].
LSD1-IN-14 (0-3 μM ;72 hours) significantly upregulates the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner[1].
LSD1-IN-14 (0-3 μM;72 hours) induces the apoptosis of 53.6% of A549 cells in a dose-dependent manner[1].
LSD1-IN-14 (1 mM; 60 minutes) has excellent stability in human liver microsomes and weak CYP inhibition, with T1/2 of 103.3 min and Clint(mic) of 13.4 μL/min/mg[1].

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

Cell Proliferation Assay

Cell Line: A549 and THP-1[1]
Concentration: 0-20 μM
Incubation Time: 72 hours
Result: Showed a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively.

Western Blot Analysis

Cell Line: A549 cells[1]
Concentration: 0, 0.3, 1 and 3 μM
Incubation Time: 72 hours
Result: Significantly upregulated the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner.

Apoptosis Analysis

Cell Line: A549 cells[1]
Concentration: 0, 0.3, 1 and 3 μM
Incubation Time: 72 hours
Result: Induced the apoptosis of 53.6% of cells in a dose-dependent manner.

体内研究
(In Vivo)

LSD1-IN-14 (2 mg/kg for i.v., 10 mg/kg for i.g, single) has an acceptable half-life and oral bioavailability[1].
Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats[1].

IV (2 mg/kg) IG (10 mg/kg)
C0 (ng/mL) 575 Cmax (ng/mL) 41.1
T1/2 (h) 1.0 T1/2 (h) 2.8
Vdss (L/kg) 6.6 Tmax (h) 0.8
Cl (mL/min/kg) 156 AUC0-t (ng.h/mL) 126
AUC0-t (ng.h/mL) 211 AUC0-∞ (ng.h/mL) 152
AUC0-∞ (ng.h/mL) 214 Bioacailability (%) 11.9

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

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 2 mg/kg for i.v., 10 mg/kg for i.g.
Administration: i.v. and i.g, single
Result: Showed an acceptable half-life and oral bioavailability.

分子量

365.45

Formula

C21H24FN5
CAS 号

2698340-11-1
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]. Wang X, et al. Design, synthesis and biological evaluation of 2-aminopyrimidine-based LSD1 inhibitors. Bioorg Chem. 2022;121:105699.

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FLT3/CDK4-IN-1

发表于由

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。

FLT3/CDK4-IN-1 

FLT3/CDK4-IN-1 是一种有效的、高选择性且具有口服活性的 FLT3/CDK4 双重抑制剂 (FLT3 与 CDK4 的 IC50 为 7 和 11 nM)。FLT3/CDK4-IN-1 对某些癌细胞具有抗增殖活性，在体内具有良好的抗肿瘤作用。

FLT3/CDK4-IN-1

FLT3/CDK4-IN-1 Chemical Structure

CAS No. : 2762296-44-4

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生物活性

FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo[1].

IC50 & Target

CDK4

7 nM (IC50)

体外研究
(In Vitro)

FLT3/CDK4-IN-1 (compound 23k) (various concentrations; 72 hours) has better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively[1].
FLT3/CDK4-IN-1 (12.5-200 nM; 24 hours) arrests the cell cycle in G1 phase in a concentration-dependent manner[1].
FLT3/CDK4-IN-1 (200-3200 nM; 48 hours) induces apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and is more capable in MV4-11 than HCT-116[1].
FLT3/CDK4-IN-1 (0-100 nM; 2hours) inhibits the phosphorylation of FLT3 at Tyr589/591 in a dose-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 Proliferation Assay

Cell Line: MV4-11, HCT-116, MDA-MB-436[1]
Concentration: Various concentrations
Incubation Time: 72 hours
Result: FLT3/CDK4-IN-1 had better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively.

Cell Cycle Analysis

Cell Line: MV4-11, HCT-116[1]
Concentration: 12.5, 25, 50, 100 and 200 nM
Incubation Time: 24 hours
Result: Arrested the cell cycle in G1 phase in a concentration-dependent manner.

Apoptosis Analysis

Cell Line: MV4-11, HCT-116[1]
Concentration: 200, 400, 800, 1600 and 3200 nM
Incubation Time: 48 hours
Result: Induced apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and was more capable in MV4-11 than HCT-116.

Western Blot Analysis

Cell Line: MV4-11[1]
Concentration: 0, 5, 10, 20, 40, 100 nM
Incubation Time: 2 hours
Result: Inhibited the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner.

体内研究
(In Vivo)

FLT3/CDK4-IN-1 (100 and 200 mg/kg; p.o.; 14 days, once daily) significantly inhibits the tumor growth at the dose of 200 mg/kg[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: Female nu/nu mice (MV4-11-injected)[1]
Dosage: 100 and 200 mg/kg
Administration: p.o.; 14 days, once daily
Result: Significantly inhibited the tumor growth at the dose of 200 mg/kg while no significant antitumor effect at 100 mg/kg.

分子量

478.54

Formula

C25H28F2N8
CAS 号

2762296-44-4
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]. Li X, et al. Synthesis and biological evaluation of 6-(pyrimidin-4-yl)-1H-pyrazolo[4,3-b]pyridine derivatives as novel dual FLT3/CDK4 inhibitors. Bioorg Chem. 2022;121:105669.

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RET-IN-8

发表于由

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。

RET-IN-8 

RET-IN-8 是一种转染期间重排激酶 (RET) 的抑制剂，可用于研究癌症，详细信息请参考专利文献 WO2021093720A1 中的化合物 I-1。

RET-IN-8

RET-IN-8 Chemical Structure

CAS No. : 2642164-75-6

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生物活性

RET-IN-8 is a rearranged during transfection (RET) kinase inhibitor extracted from patent WO2021093720A1 compound I-1. RET-IN-8 can be used for the research of cancer[1].

分子量

486.57

Formula

C27H30N6O3
CAS 号

2642164-75-6
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]. Gou J, et, al. Pyrazole[1,5-a]pyridine-3-nitrile compound and pharmaceutical use thereof. WO2021093720A1.

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ZL-Pin01

发表于由

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。

ZL-Pin01 

ZL-Pin01 是一种共价的 Pin1 的抑制剂。ZL-Pin01 显示了 Pin1-底物相互作用的有效破坏，IC50 为 1.33 μM。

ZL-Pin01

ZL-Pin01 Chemical Structure

CAS No. : 1047464-92-5

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生物活性

ZL-Pin01 is a high potent covalent Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) inhibitor. ZL-Pin01 shows potent disruption of the Pin1-substrate interaction with an IC50 of 1.33 μM[1].

分子量

328.81

Formula

C14H17ClN2O3S
CAS 号

1047464-92-5
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]. Liu L, et al. Computational and Structure-Based Development of High Potent Cell-Active Covalent Inhibitor Targeting the Peptidyl-Prolyl Isomerase NIMA-Interacting-1 (Pin1). J Med Chem. 2022;65(3):2174-2190.

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Methyl jasmonate

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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。

Methyl jasmonate 

Methyl jasmonate 是一种参与植物在逆境下防御的植物激素。Methyl jasmonate 能提高蓝莓叶提取物 (主要是花青素) 的抗氧化性能，降低AGS细胞的活力和迁移能力。具有抗癌活性。

Methyl jasmonate

Methyl jasmonate Chemical Structure

CAS No. : 1211-29-6

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100 mg ￥700 询问价格 & 货期

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生物活性

Methyl jasmonate is a phytohormone involved in plant defenses under stress conditions. Methyl jasmonate can improve antioxidant properties of blueberry leaf extracts (mainly anthocyanins), and decrease the viability and migration capacity of AGS cells. Anticarcinogenic activity[1].

体外研究
(In Vitro)

Methyl jasmonate-treated blueberry leaf extraction (10-3200 μg/mL; 1 hour) can decrease cell viability of AGS cells with increasing dose[1].
Methyl jasmonate-treated blueberry leaf extraction (10-3200 μg/mL) can significantly decrease the expression of p-P70S6K (AKT/mTOR pathway) and p-ERK1/2 (MAPK) proteins[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

Cell Line: Gastric cancer cells (line AGS)[1]
Concentration: 10, 25, 50, 100, 200, 400, 800, 1600 and 3200 μg/mL
Incubation Time: 1 hour
Result: Cell viability of AGS cells gradually decreased in response to increasing doses of blueberry leaf extract from MeJA treated plants.

Western Blot Analysis

Cell Line: AGS cells[1]
Concentration: 10, 50, 100, 200, 400, 800, 1600 and 3200 μg/mL
Incubation Time:
Result: Blueberry leaf extracts of MeJA-treated plants significantly decreased the expression of p-P70S6K (AKT/mTOR pathway) and p-ERK1/2 (MAPK) proteins.

分子量

224.30

Formula

C13H20O3
CAS 号

1211-29-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Ribera-Fonseca A, et al. The Anti-Proliferative and Anti-Invasive Effect of Leaf Extracts of Blueberry Plants Treated with Methyl Jasmonate on Human Gastric Cancer In Vitro Is Related to Their Antioxidant Properties. Antioxidants (Basel). 2020;9(1):45. Published 2020 Jan 4.

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NCT02

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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。

NCT02 

NCT02 是一种细胞周期蛋白 K 降解剂。NCT02 诱导细胞周期蛋白 K (CCNK) 的泛素化和 CCNK 及其复合物 CDK12 的蛋白酶体降解。NCT02具有研究转移性结直肠癌 (CRC) 的潜力。

NCT02

NCT02 Chemical Structure

CAS No. : 790245-61-3

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生物活性

NCT02 is a cyclin K degrader. NCT02 induces ubiquitination of cyclin K (CCNK) and proteasomal degradation of CCNK and its complex partner CDK12. NCT02 has the potential for the research of metastatic colorectal cancer (CRC)[1].

分子量

312.39

Formula

C17H16N2O2S
CAS 号

790245-61-3
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]. Dieter SM, et al. Degradation of CCNK/CDK12 is a druggable vulnerability of colorectal cancer. Cell Rep. 2021;36(3):109394.

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MIR002

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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。

MIR002 

MIR002 是一种有效且具有口服活性的 DNA polymerase α (POLA1) 和 HDAC 11 双重抑制剂。MIR002 诱导 p53 的乙酰化、p21 的激活、G1/S 细胞周期停滞和细胞凋亡apoptosis。MIR002 显示出显著的体内抗肿瘤活性。

MIR002

MIR002 Chemical Structure

CAS No. : 2217671-64-0

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生物活性

MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo[1].

IC50 & Target

HDAC11

6.09 μM (IC50)

POLA1

 

体外研究
(In Vitro)

MIR002 (24 h) shows antiproliferative activity at nanomolar concentrations (IC50s of 0.25, 2.8, 0.6, 0.41 µM in NCI-H460, H460-R9A, A2780, A2780-DX; IC50s of 0.9, 1.2, 0.22, 0.71, 2.1, 0.52, 0.038, 0.18, 0.42, 1.9, 0.64, 1.1 µM in MM432, MM473, MM487, RAMOS, L-428, U-293, Z-138, NB4, THP-1, MDA-MB231, MDA-MB436, U87MG cells, respectively)[1].
MIR002 (0.0001,0.01, 1, 10 µM) shows inhibitory activity on HDAC11 with an IC50 of 6.09 µM[1].
MIR002 (0.1, 0.25, 0.4 µM, 24 h) shows a dose-dependent p53 acetylation and p21 induction as well as H2AX Phosphorylation[1]. MIR002 (72 h) leads to cell cycle arrest at the G1-S phase[1].

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

Cell Proliferation Assay[1]

Cell Line: MM432, MM473, MM487, RAMOS, L-428, U-293, Z-138, NB4, THP-1, MDA-MB231, MDA-MB436, U87MG cells
Concentration: 10 scalar concentrations
Incubation Time: 24 h
Result: Showed antiproliferative activity at nanomolar concentrations (IC50s of 0.9, 1.2, 0.22, 0.71, 2.1, 0.52, 0.038, 0.18, 0.42, 1.9, 0.64, 1.1 µM in MM432, MM473, MM487, RAMOS, L-428, U-293, Z-138, NB4, THP-1, MDA-MB231, MDA-MB436, U87MG cells, respectively)

Western Blot Analysis[1]

Cell Line: NCI-H460, MM473, MM487, A2780 cells
Concentration: 0.1, 0.25, 0.4 µM
Incubation Time: 24 h
Result: Showed antiproliferative activity at nanomolar concentrations (IC50s of 0.9, 1.2, Showed a dosedependent p53 acetylation and p21 induction as well as H2AX Phosphorylation.

Cell Cycle Analysis[1]

Cell Line: NCI-H460, A2780, MM473, H460-R9A cells
Concentration: 0.25 µM for NCI-H460, 0.6 µM for A2780, 1.2 µM for MM473, 2.8 µM for H460-R9A
Incubation Time: 72 h
Result: Cells were arrested at the G1-S phase.

体内研究
(In Vivo)

MIR002 (50 mg/kg; p.o.; twice a day for 5 days a week, 3 weeks) shows a good tolerability and antitumor activity (TGI=61%)[1].
MIR002 (50 mg/kg; p.o.; twice a day for 5 days a week, 6 weeks) shows an additive antitumor effect with complete disappearance of tumor masses in two animals at the end of the treatment when combination with cisplatin[1].
MIR002 ( 50 mg/kg, twice a day for 5 days) induces a significant increase of a interferon at its pharmacological active dose (50 mg/kg)[1].

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

Animal Model: Model: 4-6 weeks old female CD-1 nude mice (NSCLC NCI-H460 model)
Dosage: 50 mg/kg
Administration: p.o.; twice a day for 5 days a week, 3 weeks
Result: Showed a good tolerability and antitumor activity (TGI=61%).
Animal Model: 4-6 weeks old female CD-1 nude mice ( MM473-luc and MM487-Luc)[1]
Dosage: 50 mg/kg combibnated with cisplatin (i.p.; 5 mg/kg; twice a day for 7 days a week, 6 weeks)
Administration: p.o.; twice a day for 5 days a week, 6 weeks
Result: Showed an additive antitumor effect with complete disappearance of tumor masses in two animals at the end of the treatment when combination with cisplatin.
Animal Model: 4-6 weeks old female CD-1 nude mice (Melanoma B16 model)[1]
Dosage: 50 mg/kg
Administration: p.o.; twice a day for 5 days
Result: Induced a significant increase of α interferon at its pharmacological active dose (50 mg/kg).

分子量

461.55

Formula

C28H31NO5
CAS 号

2217671-64-0
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]. Dallavalle S, et al. Antitumor activity of novel POLA1-HDAC11 dual inhibitors. Eur J Med Chem. 2022, 228:113971.

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Protein kinase inhibitor H-7

发表于由

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。

Protein kinase inhibitor H-7 

Protein kinase inhibitor H-7 是一种有效的蛋白激酶 C (PKC) 和环核苷酸依赖性蛋白激酶抑制剂，抑制 PKC的 Ki 值为 6 μM。

Protein kinase inhibitor H-7

Protein kinase inhibitor H-7 Chemical Structure

CAS No. : 84477-87-2

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生物活性

Protein kinase inhibitor H-7 is a potent inhibitor of protein kinase C (PKC) and cyclic nucleotide dependent protein kinase, with a Ki of 6 μM for PKC[1].

IC50 & Target[1]

PKC

6 μM (Ki)

分子量

291.37

Formula

C14H17N3O2S
CAS 号

84477-87-2
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]. Hidaka H, et, al. Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry. 1984 Oct 9;23(21):5036-41.

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SHP2-IN-9

发表于由

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-IN-9 

SHP2-IN-9是一种特异性的 SHP2 抑制剂 (IC50 =1.174 μM)，具有增强的血脑屏障渗透性。SHP2-IN-9 对 SHP2 的选择性是 SHP1 的 85 倍。SHP2-IN-9 在体内抑制 SHP2 介导的细胞信号转导和癌细胞增殖，并抑制宫颈癌肿瘤和胶质母细胞瘤的生长。

SHP2-IN-9

SHP2-IN-9 Chemical Structure

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生物活性

SHP2-IN-9 is a specific SHP2 inhibitor (IC50 =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo[1].

体外研究
(In Vitro)

SHP2-IN-9 (compound 2) could effectively inhibit SHP2-mediated cell signaling pathways in cancer (cervix cancer, human pancreatic cancer, large cell lung cancer and mouse glioma cell) by inhibiting the phosphorylation of Paxillin, affecting the regulation of the PI3K/AKT pathway and cell proliferation by causing the cell cycle arrest and inducing the early apoptosis[1].

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

385.46

Formula

C20H20FN3O2S
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]. Ma Y, et al. Structure-based discovery of a specific SHP2 inhibitor with enhanced blood-brain barrier penetration from PubChem database. Bioorg Chem. 2022;121:105648.

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SB-429201

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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。

SB-429201 

SB-429201 是一种有效的选择性 HDAC1 (IC50~1.5 μM)。SB-429201 对 HDAC1 抑制的偏好至少是 HDAC3 和 HDAC8 的 20 倍。

SB-429201

SB-429201 Chemical Structure

CAS No. : 1027971-34-1

规格 价格 是否有货 数量
5 mg ￥4200 In-stock
10 mg ￥6700 In-stock
25 mg ￥13500 In-stock
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SB-429201 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

SB-429201 is a potent and selective HDAC1 (IC50~1.5 μM). SB-429201 displays at least a 20-fold preference for HDAC1 inhibition over HDAC3 and HDAC8[1][2].

IC50 & Target[1]

HDAC3

1.5 μM (IC50)

分子量

436.50

Formula

C28H24N2O3
CAS 号

1027971-34-1
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
参考文献

  • [1]. Hu E, et al. Identification of novel isoform-selective inhibitors within class I histone deacetylases. J Pharmacol Exp Ther. 2003;307(2):720-728.

    [2]. Bieliauskas AV, Pflum MK. Isoform-selective histone deacetylase inhibitors. Chem Soc Rev. 2008;37(7):1402-1413.

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ZL-Pin13

发表于由

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。

ZL-Pin13 

ZL-Pin13 是一种高效细胞活性共价抑制剂，靶向 Pin1，IC50 为 67 nM。ZL-Pin13 有效抑制 MDA-MB-231 细胞的增殖并下调 Pin1 底物。

ZL-Pin13

ZL-Pin13 Chemical Structure

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生物活性

ZL-Pin13 is a high potent cell-active covalent inhibitor targeting the Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) with an IC50 of 67 nM. ZL-Pin13 effectively inhibits the proliferation and downregulated the Pin1 substrates in MDA-MB-231 cells[1].

分子量

454.97

Formula

C24H23ClN2O3S
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]. Liu L, et al. Computational and Structure-Based Development of High Potent Cell-Active Covalent Inhibitor Targeting the Peptidyl-Prolyl Isomerase NIMA-Interacting-1 (Pin1). J Med Chem. 2022;65(3):2174-2190.

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LSD1-IN-14

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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。

LSD1-IN-14 

LSD1-IN-14 是一种有效且具有选择性的 LSD1 抑制剂 (IC50=0.89 μM)。LSD1-IN-14 能显著抑制 A549 和 THP-1 细胞的增殖，能诱导肿瘤细胞的凋亡。

LSD1-IN-14

LSD1-IN-14 Chemical Structure

CAS No. : 2698340-11-1

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生物活性

LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells[1].

IC50 & Target

IC50: 0.89 μM (LSD1)[1]
体外研究
(In Vitro)

LSD1-IN-14 (compound x43) (0-20 μM; 72 hours) has a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively[1].
LSD1-IN-14 (0-3 μM ;72 hours) significantly upregulates the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner[1].
LSD1-IN-14 (0-3 μM;72 hours) induces the apoptosis of 53.6% of A549 cells in a dose-dependent manner[1].
LSD1-IN-14 (1 mM; 60 minutes) has excellent stability in human liver microsomes and weak CYP inhibition, with T1/2 of 103.3 min and Clint(mic) of 13.4 μL/min/mg[1].

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

Cell Proliferation Assay

Cell Line: A549 and THP-1[1]
Concentration: 0-20 μM
Incubation Time: 72 hours
Result: Showed a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively.

Western Blot Analysis

Cell Line: A549 cells[1]
Concentration: 0, 0.3, 1 and 3 μM
Incubation Time: 72 hours
Result: Significantly upregulated the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner.

Apoptosis Analysis

Cell Line: A549 cells[1]
Concentration: 0, 0.3, 1 and 3 μM
Incubation Time: 72 hours
Result: Induced the apoptosis of 53.6% of cells in a dose-dependent manner.

体内研究
(In Vivo)

LSD1-IN-14 (2 mg/kg for i.v., 10 mg/kg for i.g, single) has an acceptable half-life and oral bioavailability[1].
Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats[1].

IV (2 mg/kg) IG (10 mg/kg)
C0 (ng/mL) 575 Cmax (ng/mL) 41.1
T1/2 (h) 1.0 T1/2 (h) 2.8
Vdss (L/kg) 6.6 Tmax (h) 0.8
Cl (mL/min/kg) 156 AUC0-t (ng.h/mL) 126
AUC0-t (ng.h/mL) 211 AUC0-∞ (ng.h/mL) 152
AUC0-∞ (ng.h/mL) 214 Bioacailability (%) 11.9

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

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 2 mg/kg for i.v., 10 mg/kg for i.g.
Administration: i.v. and i.g, single
Result: Showed an acceptable half-life and oral bioavailability.

分子量

365.45

Formula

C21H24FN5
CAS 号

2698340-11-1
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]. Wang X, et al. Design, synthesis and biological evaluation of 2-aminopyrimidine-based LSD1 inhibitors. Bioorg Chem. 2022;121:105699.

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SOS1-IN-6

发表于由

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。

SOS1-IN-6 

SOS1-IN-6 (compound 33-P1) 是一种有效的 SOS1 抑制剂，对 SOS1-G12D 和 SOS1-G12V 的 IC50 分别为 14.9 和 73.3 nM。

SOS1-IN-6

SOS1-IN-6 Chemical Structure

CAS No. : 2751718-88-2

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生物活性

SOS1-IN-6 (compound 33-P1) is a potent SOS1 inhibitor with IC50s of 14.9 and 73.3 nM for SOS1-G12D and SOS1-G12V, respectively[1].

IC50 & Target[1]

SOS1-G12D

14.9 nM (IC50)

SOS1-G12V

73.3 nM (IC50)

分子量

471.51

Formula

C26H28F3N3O2
CAS 号

2751718-88-2
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]. Fused quinazoline derivative, preparation method therefor and application thereof in medicine. WO2021249475A1.

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Proteasome-IN-4

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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。

Proteasome-IN-4 

Proteasome-IN-4 是一种良好的非共价 proteasome 抑制剂 (IC50= 8.39 nM)。Proteasome-IN-4 对 RPMI-8226、MM-1S 和 MV-4-11 细胞系具有较强的抗增殖活性。Proteasome-IN-4 可用于癌症研究。

Proteasome-IN-4

Proteasome-IN-4 Chemical Structure

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生物活性

Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research[1].

IC50 & Target

IC50: 8.39 nM (proteasome)[1]
体外研究
(In Vitro)

Proteasome-IN-4 (compound 43) (0-20 nM; 72 hours) has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively[1].
Proteasome-IN-4 (10-1000 nM; 3 hours) causes massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM[1].
Proteasome-IN-4 (2μM) has high metabolic stability in mouse blood, with T1/2 of 329.21 min[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 Proliferation Assay

Cell Line: MM-1S, RPMI 8226 and MV-4-11 cells[1]
Concentration: 0-20 nM
Incubation Time: 72 hours
Result: Displayed potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively.

Western Blot Analysis

Cell Line: MM-1S[1]
Concentration: 10, 100 and 1000 nM
Incubation Time: 3 hours
Result: Caused massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM.

体内研究
(In Vivo)

Proteasome-IN-4 (5 mg/kg; i.v.; single) has superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h in model 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: ICR mice (6-8 weeks)[1]
Dosage: 5 mg/kg
Administration: i.v.; single
Result: Displayed superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h.

分子量

750.97

Formula

C44H58N6O5
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]. Cao Y, et al. Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment. Eur J Med Chem. 2022;233:114211.

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