RB-3

• 常用名: RB-3
• 英文名: RB-3
• CAS号: 2396639-11-3
• 分子量: 417.89
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₂₀ClN₃O₂
• 熔点: N/A
• 闪点: N/A

RB-3用途

RB-3是一种PRC1抑制剂,与RING1B-BMI1f结合,Kd为2.8μM[1]。

RB-3名称

• 英文名: RB-3

RB-3生物活性

• 描述: RB-3是一种PRC1抑制剂,与RING1B-BMI1f结合,Kd为2.8μM[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 代谢酶/蛋白酶 >> E1/E2/E3酶
• 靶点实验:

  Kd: 2.8 μM (RING1B-BMI1f)[1].

• 体外研究: RB-3可降低H2A泛素化的整体水平,并在白血病细胞系和原发性急性髓系白血病(AML)样本中诱导分化[1]。RB-3以1.6μM的IC50抑制H2A泛素化[1]。RB-3抑制PRC1并破坏与核小体的相互作用[1]。RB-3减少混合系白血病(MLL)-11-19白血病(ENL)模型中的集落形成[1]。westernblot分析[1]细胞系：TEX细胞。浓度：6,12,25μM。培养时间：8d。结果：C/EBPα-p42蛋白水平呈剂量依赖性升高。
• 参考文献:

  [1]. Shirish Shukla, et al. Small-molecule inhibitors targeting Polycomb repressive complex 1 RING domain. Nat Chem Biol. 2021 Jul;17(7):784-793.

RB-3物理化学性质

• 分子式: C₂₄H₂₀ClN₃O₂
• 分子量: 417.89
• InChIKey: IUEFQUANJWCUNT-UHFFFAOYSA-N
• SMILES: CC(C)c1c(-c2cccc3[nH]ccc23)[nH]c(C(=O)O)c1-c1c(Cl)ccc2[nH]ccc12

RB-3靶点实验

查看更多实验

实验名称：Inhibition of TRIM37 (unknown origin) activity at 12.2 to 50 uM relative to control 来源：ChEMBL 靶标：N/A External Id：CHEMBL5052906

实验名称：Inhibition of BRCA1-BARD1 (unknown origin) activity at 12.2 to 50 uM relative to cont... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5052905

实验名称：Inhibition of RING1B-PCGF1 (unknown origin) activity at 0.4 to 25 uM relative to cont... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5052904

实验名称：Inhibition of RING1B-BMI1 H2Aub activity in human TEX cells at 6 to 25 uM relative to... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5052910

实验名称：Inhibition of RING1B-BMI1 H2Aub activity in human K562 cells at 6.2 to 25 uM relative... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5052909

实验名称：Inhibition of PRC1 in human K562 cells 来源：ChEMBL 靶标：N/A External Id：CHEMBL5052908

实验名称：Inhibition of RING1B-BMI1 (unknown origin) interaction with nucleosome at 0.8 to 12.5... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5052907

实验名称：Antitumour activity against human M9-ENL1 cells transplanted in mouse assessed as dec... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5052914

实验名称：Antitumour activity against human M9-ENL1 cells transplanted in mouse assessed as dec... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5052913

实验名称：Inhibition of colony formation in human M9-ENL1 来源：ChEMBL 靶标：N/A External Id：CHEMBL5052912

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