YM281

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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。

YM281 

YM281 是一种有效的 EZH2 抑制剂。YM281 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G0/G1 期。YM281 在体内显示出抗肿瘤作用。YM281 具有研究淋巴瘤的潜力。

YM281

YM281 Chemical Structure

CAS No. : 2230914-84-6

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生物活性

YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma[1].

体外研究
(In Vitro)

YM281 (compound V2) (0-6 µM; 0-48 h) decreases the EZH2 protein level and the PRC2 (polycomb repressive complex 2) complex through the VHL (vonHippel−Lindau)-dependent ubiquitin-proteasome system[1].
YM281 (0-10 µM; 24 h) shows anticancer effects in lymphoma cells[1].
YM281 (0-5 µM) induces cell apoptosis and cell cycle arrest at the G0/G1 phase[1].
YM281 (0-5 µM; 24 h) increases the activity of caspase-3 and -7 and meanwhile reduces the cell viability in primary lymphoma cells[1].

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

Western Blot Analysis[1]

Cell Line: SU-DHL-2, 22Rv1 cells
Concentration: 0-6 µM
Incubation Time: 0-48 h
Result: Abrogated both the EZH2 protein level and the H3K27me3 degree in a concentration-dependent manner in 24 h, had no significant effect on the protein level of EZH1,and significantly increased the expression of EZH2 ubiquitination.

Cell Viability Assay[1]

Cell Line: SU-DHL-2, SU-DHL-4, SU-DHL-6 cells
Concentration: 0-10 µM
Incubation Time: 24 h
Result: Induced nearly complete cell viability inhibition.

Cell Cycle Analysis[1]

Cell Line: SU-DHL-6 cells
Concentration: 1, 3, 5 µM
Incubation Time: 24 h
Result: Induced cell cycle arrest at the G0/G1 phase and a profound sub-G1 population increasein a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: SU-DHL-6 cells
Concentration: 0-5 µM
Incubation Time: 48 h
Result: Significantly increased the expression of cleaved caspase-3 and PARP.

体内研究
(In Vivo)

YM281 (80, 100 mg/kg; i.v.; 6 times for 3 weeks) shows antitumor effects and significantly reduces the expression of EZH2 protein and H3K27me3 levels[1].

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 (SU-DHL-6 xenograft model)[1]
Dosage: 80 mg/kg
Administration: I.v.; 6 times for 3 weeks
Result: Remarkably suppressed the tumor volume and significantly reduced the EZH2 protein and H3K27me3 levels.
Animal Model: Balb/c nude mice (Jeko-1 xenograft model)[1]
Dosage: 100 mg/kg
Administration: I.v.; 6 times for 3 weeks
Result: Shows anti-tumor effects with the significantly reduced the expression of EZH2 protein and H3K27me3 levels.

分子量

1018.27

Formula

C56H71N7O9S
CAS 号

2230914-84-6
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]. Tu Y,et al. Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma. J Med Chem. 2021 Jul 22;64(14):10167-10184.

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