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MC2590
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。
MC2590图片
CAS NO:2284460-01-9
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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)

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).
分子量

347.37

Formula

C20H17N3O3

CAS 号

2284460-01-9

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.