YM458

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

YM458 

YM458 是一种有效的 EZH2 和 BRD4 双重抑制剂，对 EZH2 和 BRD4 的 IC50 分别为490 nM 和 34 nM。YM458 可抑制实体癌细胞增殖和集落形成，诱导细胞周期阻滞与细胞凋亡 (apoptosis)。YM458 可用于抗癌研究。

YM458

YM458 Chemical Structure

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生物活性

YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer[1].

IC50 & Target[1]

EZH2

490 nM (IC50)

BRD4

34 nM (IC50)

体外研究
(In Vitro)

YM458 (compound D7) (0-30 μM; 6 days) has antiproliferative activities against AsPC-1 cells with an IC50 of 0.69 ± 0.16 μM; and (1 μM; 72 hours) significantly decreases the degree of H3K27me3 and c-Myc in AsPC-1[1].
YM458 (0-30 μM; 4 or 6 days) inhibits cell proliferation on a broad range of solid cancer cells, and significantly suppresses proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM[1].
YM458 (0.05-0.4 μM; 12-20 days) inhibits colony formation of AsPC-1, HCT116, and A549 cancer cells in a dose-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line: AsPC-1[1]
Concentration: 1 μM
Incubation Time: 72 hours
Result: Decreased the degree of H3K27me3 and c-Myc significantly.

Cell Proliferation Assay

Cell Line: AsPC-1, SW1990, CFPAC-1, A549, HCC827, H1650, H292, H460, DLD1, HCT116, and RKO[1]
Concentration: 0-30 μM
Incubation Time: 4 or 6 days
Result: Inhibited cell proliferation on a broad range of solid cancer cells, and significantly suppressed proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM.

体内研究
(In Vivo)

YM458 (60 mg/kg; IP; every other day, for 38 days) prevents tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells[1].
Pharmacokinetic Parameters of YM458 in Female BALB/c mice[1].

IP (80 mg/kg) PO (80 mg/kg)
t1/2 (h) 3.81 4.16
Tmax (h) 1 1
Cmax (ng/mL) 27126.3 4383.6
AUC0-24 (ng/mL·h) 273220.1 13509.1
CL (mL/min/kg) 4.88
F (%) 4.94

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice (injected with A549 or AsPC-1)[1]
Dosage: 60 mg/kg
Administration: IP; every other day, for 38 days
Result: Prevented tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells.

分子量

957.62

Formula

C53H61ClN8O5S
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.
参考文献

  • [1]. Guo Z, et al. Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors. J Med Chem. 2022;65(9):6573-6592.

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