2. Cell Cycle/DNA Damage Epigenetics
  3. PARP Histone Methyltransferase
  4. PARP/EZH2-IN-2

PARP/EZH2-IN-2 (compound 12e) 是一种双靶点 PARP1 和 EZH2 抑制剂，IC50 值分别为 6.89 和 27.34 nM。PARP/EZH2-IN-2 显示出抗癌活性，对正常细胞没有毒性。PARP/EZH2-IN-2 通过抑制 EZH2 去增加对 PARP1 的敏感性来间接实现合成致死，并通过调节过度自噬诱导细胞死亡。

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PARP/EZH2-IN-2 Chemical Structure

PARP/EZH2-IN-2 Chemical Structure

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Customer Review

PARP/EZH2-IN-2 相关抗体

Top Publications Citing Use of Products

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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

PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy[1].

IC50 & Target

PARP1

6.89 ± 0.7 nM (IC50)

EZH2

27.34 ± 1. nM (IC50)

体外研究
(In Vitro)

PARP/EZH2-IN-2 (compound 12e) 对 MDA-MB-231 细胞 (IC50=2.84 μM) 和 BT-549 细胞 (IC50=0.91 μM) 显示出最佳的细胞毒性，对正常乳腺细胞系没有毒性[1]。

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

PARP/EZH2-IN-2 相关抗体:
体内研究
(In Vivo)

PARP/EZH2-IN-2 (compound 12e) (20-50 mg/kg, 腹腔注射) 表现出良好的抗肿瘤活性，优于 Niraparib (HY-10619) + GSK126 (HY-13470)[1]。

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

Animal Model: Female BALB/c nude mice (5 weeks after birth, MDA-MB-231 cells subcutaneous injection)[1]
Dosage: 20, 50 mg/kg
Administration: Intraperitoneally for 21 consecutive days
Result: Significantly suppressed tumor growth and downregulated the expression of the PARP1/EZH2 protein in tumor tissues at a dose of 50 mg/kg.
分子量

573.64

Formula

C33H31N7O3
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

PARP/EZH2-IN-2 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 *
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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:

PARP/EZH2-IN-2PARPHistone Methyltransferasepoly ADP ribose polymeraseTriple-negative breast cancerMDA-MB-231 cellsBT-549 cellsInhibitorinhibitorinhibit

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