MC2625 是一种有效的含吡啶的组蛋白脱乙酰酶 (HDAC) 抑制剂。MC2625 显示选择性 HDAC3 和 HDAC6 抑制作用，IC50分别为 80 nM 和 11 nM。MC2625 增加乙酰-H3 和乙酰-微管蛋白水平，并通过细胞凋亡诱导抑制癌症干细胞 (CSC) 的生长。
| 生物活性 | MC2625 is a potent pyridine-containinghistone deacetylase (HDAC)inhibitor. MC2625 show selectiveHDAC3andHDAC6inhibition withIC50s of 80 nM and 11 nM. MC2625 increases acetyl-H3 and acetyl-tubulin levels and inhibitscancer stem cells(CSCs) growth byapoptosisinduction[1][2]. |
| IC50& Target[1][2] | 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) |
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体外研究
(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. |
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| 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. |
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