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PRT4165 {[allProObj[0].p_purity_real_show]}

货号：A295342 同义名： NSC600157

PRT4165, an inhibitor of bim1 and ring1A, could block PRC1 (Polycomb-repressive complex 1)-mediated H2A ubiquitylation.

PRT4165 化学结构 CAS号：31083-55-3
PRT4165 化学结构
CAS号：31083-55-3
PRT4165 3D分子结构
CAS号：31083-55-3
PRT4165 化学结构 CAS号：31083-55-3
PRT4165 3D分子结构 CAS号：31083-55-3
规格 价格 会员价 库存 数量
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PRT4165 纯度/质量文件 产品仅供科研

货号：A295342 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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PRT4165 生物活性

靶点

  • E3 Ligase

    Bmi1/Ring1A, IC50:3.9 μM
描述 Polycomb-repressive complex 1 (PRC1) is a histone H2A/H2AX E3 ubiquitin ligase. PRC1 has a critical role in the regulation of differentiation and the maintenance of stem cell populations[2]. PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation that inhibits the PRC1 subunits BMI1/RING1 with IC50 value of 3.9μM[3]. In vitro, treatment with 50μM PRT4165 in A375 cells or 100μM in Hela cells for 3h leaded to disappearance of the speckled staining in the nuclei and appearance of Bmi1 also in the cytoplasm[3]. PRT4165 inhibited H2AUB and sphere formation with IC50 values of 3.52mM and 1.05mM in PC3 cells [4]. Treatment PRT4165 at dose of 50μM PRT4165 suppressed growth of leukemia cell lines THP-1, TMD7, OCI/AML772, OCI/AML5, Jurkat and KOPT-K1 by apoptosis. In addition, PRT4165 inhibited the expression of NOTCH1 in KOPT-K1, OCI/ALML2 and OCI/AML5 cells. PRT4165 also inhibited the expression of NOTCH1, MYC, and HES1 in KOPT-K1 cells[5]. In vivo, administration of 8mg/kg PRT4165 caused disruption of decidualization and polyploidy development during early pregnancy by inhibition of PRC1 in mice[6].
作用机制 PRT4165 inhibits PRC1-mediated histone H2A ubiquitylation and the accumulation of ubiquitin at the DNA double-strand break sites [2].

PRT4165 参考文献

[1]Ismail IH, McDonald D, et al. A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks. J Biol Chem. 2013 Sep 13;288(37):26944-54.

[2] Ismail IH. A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks. J Biol Chem. 2013 Sep 13;288(37):26944-54. doi: 10.1074/jbc.M113.461699. Epub 2013 Jul 30.

[3] Alchanati I. The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2alpha cleavage complex - a potentially new drug target. PLoS One. 2009 Dec 1;4(12):e8104. doi: 10.1371/journal.pone.0008104.

[4]Su W. The Polycomb Repressor Complex 1 Drives Double-Negative Prostate Cancer Metastasis by Coordinating Stemness and Immune Suppression. Cancer Cell. 2019 Aug 12;36(2):139-155.e10. doi: 10.1016/j.ccell.2019.06.009. Epub 2019 Jul 18.

[5]Ohtaka M, Itoh M, Tohda S. BMI1 Inhibitors Down-regulate NOTCH Signaling and Suppress Proliferation of Acute Leukemia Cells. Anticancer Res. 2017 Nov;37(11):6047-6053. doi: 10.21873/anticanres.12052.

[6]Bian F. Polycomb repressive complex 1 controls uterine decidualization. Sci Rep. 2016 May 16;6:26061. doi: 10.1038/srep26061.

PRT4165 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.25mL

0.85mL

0.43mL

21.26mL

4.25mL

2.13mL

42.51mL

8.50mL

4.25mL

PRT4165 技术信息

CAS号31083-55-3
分子式C15H9NO2
分子量 235.238
别名 NSC600157
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C
溶解度

DMSO: 25 mg/mL(106.28 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: PRT4165 | 31083-55-3 | NSC600157 | PRT 4165 | PRT-4165 | NSC 600157 | NSC-600157 | E1/E2/E3 Enzyme Inhibitor | Metabolic Enzyme/Protease | E1/E2/E3 Enzyme | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | PRT4165 纯度/质量文件 | PRT4165 生物活性 | PRT4165 参考文献 | PRT4165 实验方案 | PRT4165 技术信息

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