HDAC-IN-37

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。

HDAC-IN-37 

HDAC-IN-37 是一种有效的 HDAC 抑制剂，对 HDAC1、HDAC3、HDAC8 和 HDAC6 的 IC50 分别为 0.0551 μM、1.24 μM、0.948 μM 和 34.2 μM。HDAC-IN-37 能缓慢诱导组蛋白乙酰化。HDAC-IN-37 抑制细胞由 G1 期向 S 期转变，诱导早期细胞凋亡 (apoptosis)。

HDAC-IN-37

HDAC-IN-37 Chemical Structure

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生物活性

HDAC-IN-37 is a potent HDAC inhibitor with IC50s of 0.0551 μM, 1.24 μM, 0.948 μM and 34.2 μM for HDAC1, HDAC3, HDAC8 and HDAC6, respectively. HDAC-IN-37 induces histone acetylation in a slow-off manner. HDAC-IN-37 prevents cell transition from G1 phase to S phase and induces early cell apoptosis[1].

IC50 & Target[1]

HDAC1

55.1 nM (IC50)

HDAC3

1.24 μM (IC50)

HDAC8

0.948 μM (IC50)

HDAC6

34.2 μM (IC50)

体外研究
(In Vitro)

HDAC-IN-37 (compound 9d) exhibits the potent antiproliferative activities on the HCT116, MDA-MB-231, K562 cell lines at IC50s of 0.50, 0.38, 0.12 μM, respectively[1].
HDAC-IN-37 (0 – 10 μM; 24 hours) significantly induces the accumulation of acetylated histones at H3K9 and H4K5 in HCT-116 cells[1].
HDAC-IN-37 (0 – 10 μM; 24 hours) induces cell apoptosis in HCT-116 cells by 35.22%, 58.34, 80.7% at 0.5, 1, 5 μM, mainly occurring in early apoptosis[1].
HDAC-IN-37 (0 – 10 μM; 6, 12, 24 hours) causes G0/G1 phase arrest of HCT-116 cells in a time-dependent manner, effectively preventing cell cycle progression[1].
HDAC-IN-37 (0, 0.1, 0.5, 1, 5 and 10 μM; 0, 6, 12, 24, 36, 48 hours) down-regulates the levels of CDK2, Cyclin D1 and the up-regulates P21 with dose- and time-dependent manners in HCT-116 cells, and decreases Bcl-2 of Bcl-2 family in dose- and time-dependent manners[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: HCT-116, MDA-MB-231, HepG2, A549, SGC7901 and K562[1]
Concentration: 0-10 μM
Incubation Time: 48 hours
Result: Exhibited the potent antiproliferative activities on the HCT116, MDA-MB-231, K562 cell lines at IC50 of 0.50, 0.38, 0.12 μM, respectively.

Western Blot Analysis

Cell Line: HCT-116[1]
Concentration: 0, 0.1, 0.5, 1, 5 and 10 μM
Incubation Time: 24 hours
Result: Significantly induced the accumulation of acetylated histones at H3K9 and H4K5 in HCT-116 cells.

Apoptosis Analysis

Cell Line: HCT-116[1]
Concentration: 0.1, 0.5, 1, 5 and 10 μM
Incubation Time: 24 hours
Result: Induced cell apoptosis in HCT-116 cells by 35.22%, 58.34, 80.7% at 0.5, 1, 5 μM, mainly occurring in early apoptosis.

Cell Cycle Analysis

Cell Line: HCT-116[1]
Concentration: 0.1, 0.5, 1, 5 and 10 μM
Incubation Time: 0, 6, 12 and 24 hours
Result: Caused G0/G1 phase arrest of HCT-116 cells in a time-dependent manner, effectively preventing cell cycle progression.

分子量

449.94

Formula

C23H24ClN7O
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]. Mao PT, He WB, Mai X, et al. Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. Bioorg Med Chem.

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