MC2590 是一种有效的含吡啶的组蛋白脱乙酰酶 (HDAC) 抑制剂。MC2590 是 HDAC1-3、-6、-8 和 -10 的抑制剂 (I/IIb 类选择性抑制剂)，IC50为 0.015 μM-0.156 μM。MC2590 还抑制其他 HDAC 亚型, HDAC4、HDAC5、HDAC7 、HDAC9、HDAC11，IC50为 1.35 μM-3.98 μM。MC2625 诱导 G2/M 细胞周期停滞并调节促凋亡和抗凋亡 microRNA 以诱导细胞凋亡。
| 生物活性 | MC2590 is a potent pyridine-containinghistone deacetylase (HDAC)inhibitor. MC2590 is a inhibitor of HDAC1-3, -6, -8, and -10 (class I/IIb-selective inhibitor) withIC50s of 0.015 μM-0.156 μM. MC2590 also inhibitsHDACisoformsHDAC4,HDAC5,HDAC7,HDAC9,HDAC11with IC50s of 1.35 μM-3.98 μM. MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptoticmicroRNAstowardsapoptosisinduction[1]. |
| IC50& Target[1] | HDAC1 0.098 μM (IC50) | HDAC2 0.156 μM (IC50) | HDAC3 0.039 μM (IC50) | HDAC6 0.015 μM (IC50) | HDAC8 0.047 μM (IC50) | HDAC10 0.071 μM (IC50) | HDAC4 2.73 μM (IC50) | HDAC5 1.35 μM (IC50) | HDAC7 2.06 μM (IC50) | HDAC9 2.79 μM (IC50) | HDAC11 3.98 μM (IC50) |
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体外研究
(In Vitro) | MC2625 (化合物5e; 72 小时) 抑制结直肠癌细胞 HCT116 (IC50=0.07 μM)、肺腺癌细胞 A549 (IC50=0.32 μM)、慢性粒细胞白血病 K562 (IC50=0.05 μM)[1]。
MC2625 (1, 5 μM; 24, 48 小时) 诱导 G2/M 细胞周期停滞[1]。
MC2625 (1, 5 μM; 24, 48 小时) 诱导 H3K9/14 过度乙酰化活性，增加乙酰-α-微管蛋白水平，显着上调 p21 蛋白[1]。
MC2625 (1, 5 μM; 48 小时) 增加 p21、BAX 和 BAK 的 mRNA 表达，下调细胞周期蛋白 D1 和 BCL-2，并调节促凋亡和抗凋亡 microRNA 以诱导细胞凋亡[1]。
Cell Cycle Analysis[1] | Cell Line: | Human acute myeloid leukaemia U937 cells | | Concentration: | 1, 5 μM | | Incubation Time: | 24, 48 h | | Result: | At 24 h, showed very low increase of the pre-G1 peak and led to a G2/M phase arrest at 1 μM; induced a 10% pre-G1 increase and displayed a block at the G2/M phase at 5 μM.
At 48 h, induced a 70-85% block of the cell cycle at the G1 phase. |
Western Blot Analysis[1] | Cell Line: | Human acute myeloid leukaemia U937 cells | | Concentration: | 1, 5 μM | | Incubation Time: | 24, 48 h | | Result: | At 1 μM revealed H3K9/14 hyperacetylation activity, increased the acetyl-α-tubulin level, markedly upregulated the p21 protein. |
RT-PCR[1] | Cell Line: | Human acute myeloid leukaemia U937 cells | | Concentration: | 1, 5 μM | | Incubation Time: | 48 h | | Result: | At 1 μM significantly induced the expression of BAX and BAK, dose-dependently downregulated the antiapoptotic factor BCL-2.
Downregulated miRNAs with antiapoptotic activity (miR-17-5p, miR-18-5p, miR-19b-3p, miR-20a-5p, miR-21-5p); induced the proapoptotic miRNAs (miR-let7a-5p, miR-125b-5p, miR-181a-5p, miR-181b-5p, miR-769-5p, miR-122-5p). |
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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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