SGC-SMARCA-BRDVIII

• 常用名: SGC-SMARCA-BRDVIII
• 英文名: SGC-SMARCA-BRDVIII
• CAS号: 1997319-84-2
• 分子量: 371.43
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₉H₂₅N₅O₃
• 熔点: N/A
• 闪点: N/A

SGC-SMARCA-BRDVIII用途

SGC-SMARCA-BRDVIII是SMARCA2/4和PB1(5)的有效和选择性抑制剂,Kds分别为35 nM、36 nM和13 nM。SGC-SMARCA-BRDVIII也抑制PB1(2)和PB1(3),Kds分别为3.7和2.0μM。SGC-SMARCA-BRDVIII可阻断3T3-L1小鼠成纤维细胞的脂肪生成[1][2]。

SGC-SMARCA-BRDVIII名称

• 英文名: SGC-SMARCA-BRDVIII

SGC-SMARCA-BRDVIII生物活性

• 描述: SGC-SMARCA-BRDVIII是SMARCA2/4和PB1(5)的有效和选择性抑制剂,Kds分别为35 nM、36 nM和13 nM。SGC-SMARCA-BRDVIII也抑制PB1(2)和PB1(3),Kds分别为3.7和2.0μM。SGC-SMARCA-BRDVIII可阻断3T3-L1小鼠成纤维细胞的脂肪生成[1][2]。
• 相关类别:
  研究领域 >> 代谢疾病
  信号通路 >> 表观遗传学 >> 表观遗传读者域
• 靶点实验:

  Kd: 35 nM (SMARCA2), 36 nM (SMARCA4), 13 nM (PB1(5))[1]

• 体外研究: SGC-SMARCA-BRDVIII(化合物22)(1μM；14天)阻断3T3-L1小鼠成纤维细胞中的脂肪细胞分化[1]。
• 参考文献:

  [1]. Wanior M, et, al. Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. J Med Chem. 2020 Dec 10;63(23):14680-14699.

  [2]. Mélin L, et, al. Design and Synthesis of LM146, a Potent Inhibitor of PB1 with an Improved Selectivity Profile over SMARCA2. ACS Omega. 2021 Aug 9;6(33):21327-21338.

SGC-SMARCA-BRDVIII物理化学性质

• 分子式: C₁₉H₂₅N₅O₃
• 分子量: 371.43
• 储存条件: -20°C

SGC-SMARCA-BRDVIII安全信息

• 危害码 (欧洲): Xn

SGC-SMARCA-BRDVIII靶点实验

查看更多实验

实验名称：Thermal Shift Assay. Domain start/stop: M626-G740 来源：ChEMBL 靶标：Peregrin External Id：CHEMBL4650107

实验名称：Thermal Shift Assay. Domain: start/stop: M1-L298 来源：ChEMBL 靶标：Cyclin-dependent kinase 2 External Id：CHEMBL5062802

实验名称：Thermal Shift Assay. Domain: start/stop: M26-R383 来源：ChEMBL 靶标：Glycogen synthase kinase-3 beta External Id：CHEMBL5065589

实验名称：Thermal Shift Assay. Domain: start/stop: S229-K512 来源：ChEMBL 靶标：Tyrosine-protein kinase ABL1 External Id：CHEMBL5060015

实验名称：Binding affinity to polybromo-1 (2) (unknown origin) by ITC analysis 来源：ChEMBL 靶标：Protein polybromo-1 External Id：CHEMBL4677784

实验名称：Binding affinity to polybromo-1 (3) (unknown origin) by ITC analysis 来源：ChEMBL 靶标：Protein polybromo-1 External Id：CHEMBL4677783

实验名称：Binding affinity to SMARCA2 (unknown origin) assessed as change in melting temperatur... 来源：ChEMBL 靶标：Probable global transcription activator SNF2L2 External Id：CHEMBL4677786

实验名称：Binding affinity to SMARCA4 (unknown origin) assessed as change in melting temperatur... 来源：ChEMBL 靶标：Transcription activator BRG1 External Id：CHEMBL4677785

实验名称：Toxicity in human MDA-MB-231 cells assessed as effect on cell viability up to 50 uM a... 来源：ChEMBL 靶标：MDA-MB-231 External Id：CHEMBL4677772

实验名称：Toxicity in human MDA-MB-231 cells assessed as effect on cell viability up to 50 uM a... 来源：ChEMBL 靶标：MDA-MB-231 External Id：CHEMBL4677771

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