2. Cell Cycle/DNA Damage Epigenetics Apoptosis Immunology/Inflammation
  3. PARP Histone Methyltransferase Apoptosis Pyroptosis Necroptosis
  4. PARP1/EZH2-IN-1

PARP1/EZH2-IN-1 是一种选择性的 PARP1 和 EZH2 双重抑制剂。它对 PARP1、PARP2和 EZH2 的 IC50 值分别为 28 nM、 414 nM 和 74 nM。PARP1/EZH2-IN-1能抑制 TNBC 细胞 (三阴性乳腺癌细胞) 的增殖与迁移。它可诱导 PANoptosis (一种同时包含细胞凋亡、焦亡和坏死性凋亡的细胞死亡形式) ，提高 reactive oxygen species 水平，并激活相关的炎症通路。PARP1/EZH2-IN-1 可用于三阴性乳腺癌的相关研究。

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PARP1/EZH2-IN-1

PARP1/EZH2-IN-1 Chemical Structure

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PARP1/EZH2-IN-1 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 ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 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

PARP1/EZH2-IN-1 is a selective PARP1 and EZH2 dual inhibitor. PARP1/EZH2-IN-1 has IC50s of 28 nM, 414 nM and 74 nM for PARP1, PARP2 and EZH2, respectively. PARP1/EZH2-IN-1 inhibits the proliferation and migration of TNBC cells (triple-negative breast Cancer cells). PARP1/EZH2-IN-1 induces PANoptosis (Apoptosis, Pyroptosis and Necroptosis), increases the level of reactive oxygen species, and activates related inflammatory pathways. PARP1/EZH2-IN-1 can be used in triple-negative breast cancer research[1].

IC50 & Target

PARP-1

28 nM (IC50)

PARP2

414 nM (IC50)

EZH2

74 nM (IC50)

体外研究
(In Vitro)

PARP1/EZH2-IN-1 (compound PE32) (0.5-2.0 μM, 48 h) 可抑制 MDA-MB-231 与 BT-549 的增殖和生长[1]。
PARP1/EZH2-IN-1 (2.0 μM, 48 h)可导致 BT-549 细胞中DNA损伤加剧，并破坏同源重组修复通路[1]。
PARP1/EZH2-IN-1 (1.5 μM, 48 h) 通过诱导细胞的凋亡和焦亡导致 BT-549 细胞死亡[1]。
PARP1/EZH2-IN-1 (48 h, 0.625-10 μM) 主要通过触发 ROS 爆发发挥其抗肿瘤效应[1]。
PARP1/EZH2-IN-1 能显著富集与肿瘤相关的死亡通路 (如癌症中的转录失调、 ECM 受体相互作用和TNF 信号通路），激活关键炎症通路 (如 IL-17 和 NF-κB )，并通过激活这些关键炎症信号级联反应诱导肿瘤细胞发生焦亡[1]。

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

PARP1/EZH2-IN-1 相关抗体:

Cell Invasion Assay[1]

Cell Line: BT-549 cells
Concentration: 1.0, 1.5 and 2.0 μM
Incubation Time: 24 h
Result: Inhibited the invasion of TNBC cells.
Suppressed cell migration in scratch-wound repair.

Cell Invasion Assay[1]

Cell Line: BT-549 cells
Concentration: 1.0, 1.5 and 2.0 μM
Incubation Time: 24 h
Result: Inhibited the invasion of TNBC cells.
Suppressed cell migration in scratch-wound repair.
Exhibited a stronger inhibitory effect on TNBC cells

Western Blot Analysis[1]

Cell Line: BT-549 cells
Concentration: 2.0 μM
Incubation Time: 48 h
Result: Decreased the expression levels of PAR, H3K27me3, BRCA1 and RAD51 proteins.
Increased the expression level of γ-H2AX.

Cell Viability Assay[1]

Cell Line: TNBC cell
Concentration: 0.625, 1.25, 2.5, 5, 10μM
Incubation Time: 48 h
Result: Suppressed TNBC cell viability in a manner dependent on ROS accumulation, as evidenced by the significant reversal of this effect upon co-treatment with the ROS scavenger NAC.
分子量

723.26

Formula

C39H43ClN8O4
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

PARP1/EZH2-IN-1 相关分类

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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:

PARP1/EZH2-IN-1PARPHistone MethyltransferaseApoptosisPyroptosisNecroptosispoly ADP ribose polymerase breast cancerPANoptosisPARP1EZH2Inhibitorinhibitorinhibit

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