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HDAC-IN-37
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HDAC-IN-37图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
HDAC-IN-37 是一种有效的HDAC抑制剂,对HDAC1HDAC3HDAC8HDAC6IC50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)。
生物活性

HDAC-IN-37 is a potentHDACinhibitor withIC50s of 0.0551 μM, 1.24 μM, 0.948 μM and 34.2 μM forHDAC1,HDAC3,HDAC8andHDAC6, 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 cellapoptosis[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].

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 IC50of 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.