Name | MC2625 |
---|
Description | MC2625 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2625 show selective HDAC3 and HDAC6 inhibition with IC50s of 80 nM and 11 nM. MC2625 increases acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells (CSCs) growth by apoptosis induction[1][2]. |
---|---|
Related Catalog | |
Target |
HDAC3:80 nM (IC50) HDAC6:11 nM (IC50) HDAC1:1.42 μM (IC50) HDAC2:1.77 μM (IC50) HDAC4:11.7 μM (IC50) HDAC5:9.37 μM (IC50) HDAC7:8.77 μM (IC50) HDAC8:0.61 μM (IC50) HDAC9:10.6 μM (IC50) HDAC10:1.8 μM (IC50) HDAC11:10.2 μM (IC50) |
In Vitro | MC2625 (0.5-2 μM; 24-72 小时) 在 72 h 后对不同的肉瘤癌症干细胞 (CSCs) 具有有效的抗增殖作用[1]。 MC2625 (0.5-2 μM; 48 小时) 显着诱导所有 CSC 培养物的细胞凋亡,A204 CSCs 除外[1]。 MC2625 (0.5, 2 μM; 24 小时) 引起乙酰组蛋白 H3 的剂量依赖性增加[1]。 Cell Proliferation Assay[1] Cell Line: Cancer stem cells (HOS, MG-63, RD, A204, SK-ES-1, A673) Concentration: 0.5, 1, 2 μM Incubation Time: 24, 48, 72 h Result: Significantly affected MG-63, RD, and SK-ES-1 viability in 0.5 μM, while all CSCs were sensitive at 1 and 2 μM. Apoptosis Analysis[1] Cell Line: Cancer stem cells (HOS, MG-63, RD, A204, SK-ES-1, A673) Concentration: 0.5, 1, 2 μM Incubation Time: 48 h Result: Significantly induced apoptosis of all CSC cultures, with the exception of A204 CSCs. Generated an increase of the presence of apoptotic cells with concentrated dense granular fluorescence compared to untreated cells, especially at 1 and 2 μM. Western Blot Analysis[1] Cell Line: MG-63 cancer stem cells Concentration: 0.5, 2 μM Incubation Time: 24 h Result: Caused a dose-dependent increase of acetyl-histone H3. |
References |
Molecular Formula | C23H21N3O3 |
---|---|
Molecular Weight | 387.43 |