c-Met/HDAC-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。

c-Met/HDAC-IN-2 

c-Met/HDAC-IN-2 是一种高效的 c-MetHDAC 双重抑制剂,对 HDAC1c-MetIC50 分别为 18.49 nM 和 5.40 nM。c-Met/HDAC-IN-2 对几种癌细胞具有抗增殖活性。c-Met/HDAC-IN-2 能将 HCT-116 细胞周期阻滞在 G2/M 期,诱导细胞凋亡 (apoptosis)。c-Met/HDAC-IN-2 可用于抗癌耐药研究。

c-Met/HDAC-IN-2

c-Met/HDAC-IN-2 Chemical Structure

CAS No. : 2740495-53-6

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生物活性

c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance[1].

IC50 & Target[1]

HDAC1

18.49 nM (IC50)

c-Met

5.4 nM (IC50)

体外研究
(In Vitro)

c-Met/HDAC-IN-2 (compound 14X) (0-20 μM; 72 hours) exhibits antiproliferative activities against HCT-116, MCF-7 and A549[1].
c-Met/HDAC-IN-2 (0.2-5 μM; 48 hours) induces of cancer cell apoptosis in a dose-dependent manner[1].
c-Met/HDAC-IN-2 (0.2-5 μM; 48 hours) significantly causes G2/M-phase arrest in HCT-116 cells in a dose dependent manner[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: HCT-116, MCF-7 and A549[1]
Concentration: 0-20 μM
Incubation Time: 72 hours
Result: Exhibited antiproliferative activities against HCT-116, MCF-7 and A549 with IC50s of 0.22 ± 0.09 μM, 1.59 ± 0.06 μM and 0.22 ± 0.04 μM, respectively.

Apoptosis Analysis

Cell Line: HTC-116[1]
Concentration: 0.2, 1 and 5 μM
Incubation Time: 48 hours
Result: The percentage of apoptotic cells was 4.19%, 11.53% and 21.48% at 0.2 μM, 1.0 μM and 5.0 μM, respectively.

Cell Cycle Analysis

Cell Line: HTC-116[1]
Concentration: 0.2, 1 and 5 μM
Incubation Time: 48 hours
Result: Significantly caused G2/M-phase arrest in HCT-116 cells in a dose dependent manner.

分子量

623.66

Formula

C34H33N5O7

CAS 号

2740495-53-6

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]. Hu H, Chen F, Dong Y, et al. Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors. Eur J Med Chem. 2020;204:112651.

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