MC1742 是一种有效的HDAC抑制剂，对 HDAC1、HDAC2、HDAC3、HDAC6、HDAC8、HDAC10 和 HDAC11 的IC50分别为 0.1 μM、0.11 μM、0.02 μM、0.007 μM、0.61 μM、0.04 μM 和 0.1 μM。MC1742 可以增加乙酰 - H3 和乙酰微管蛋白的水平，抑制癌症干细胞 (CSC) 的生长。MC1742 可诱导肉瘤干细胞生长停滞、凋亡 (apoptosis) 和分化。
| 生物活性 | MC1742 is a potentHDACinhibitor, withIC50s of 0.1 μM, 0.11 μM, 0.02 μM, 0.007 μM, 0.61 μM, 0.04 μM and 0.1 μM forHDAC1,HDAC2,HDAC3,HDAC6,HDAC8,HDAC10andHDAC11, respectively. MC1742 can increase acetyl-H3 and acetyl-tubulin levels and inhibitscancer stem cellsgrowth. MC1742 can induce growth arrest,apoptosis, and differentiation in sarcoma CSC[1]. |
| IC50& Target[1] | HDAC1 0.1 μM (IC50) | HDAC2 0.11 μM (IC50) | HDAC3 0.02 μM (IC50) | HDAC6 0.007 μM (IC50) | HDAC8 0.61 μM (IC50) | HDAC10 0.04 μM (IC50) | HDAC11 0.1 μM (IC50) |
|
体外研究
(In Vitro) | MC1742 (compound 1) (0.5 and 2 μM; 24 hours) increases acetylation in a dose-dependent manner, observable as punctuate nuclear staining of acetyl-histone H3[1].
MC1742 (0.5, 1 and 2 μM; 24, 48 and 72 hours) significantly induces apoptosis of all CSC cultures[1].
MC1742 (0.025-0.5 μM; 14 days) enhances bone nodule formation in a significant dose-dependent manner[1].
Immunofluorescence | Cell Line: | Sarcoma cancer stem cells[1] | | Concentration: | 0.5 and 2 μM | | Incubation Time: | 24 hours | | Result: | Increased acetylation in a dose-dependent manner, observable as punctuate nuclear staining of acetyl-histone H3. |
Apoptosis Analysis | Cell Line: | Sarcoma cancer stem cells[1] | | Concentration: | 0.5, 1 and 2 μM | | Incubation Time: | 24, 48 and 72 hours | | Result: | Significantly induced apoptosis of all CSC cultures. |
Cell Differentiation Assay | Cell Line: | Sarcoma cancer stem cells[1] | | Concentration: | 0.025, 0.05, 0.1 and 0.5 μM | | Incubation Time: | 14 days | | Result: | Successfully enhanced bone nodule formation in a significant dose-dependent manner. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 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. |
m.cnreagent.com