2. Apoptosis Epigenetics
  3. Apoptosis Histone Methyltransferase
  4. 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。

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YM281 Chemical Structure

YM281 Chemical Structure

CAS No. : 2230914-84-6

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YM281 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

YM281 相关抗体:

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].

MCE 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
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.
纯度 & 产品资料
参考文献

YM281 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YM2812230914-84-6YM 281YM-281ApoptosisHistone MethyltransferaseSU-DHL-6 xenograftlymphomaantitumorapoptosisG0/G1SU-DHL-6 cellscleaved caspase-3ubiquitin-proteasomeInhibitorinhibitorinhibit

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