中文名称:
GSK1324726A (I-BET726)
中文同义词:
4-[(2S,4R)-1-乙酰基-4-[(4-氯苯基)氨基]-2-甲基-1,2,3,4-四氢-6-喹啉基]苯甲酸;BET蛋白抑制剂(GSK1324726A);4-((2S,4R)-1-乙酰基-4-((4-氯苯基)氨基)-2-甲基-1,2,3,4-四氢喹啉-6-基)苯甲酸;化合物GSK1324726A
英文名称:
GSK1324726A (I-BET726)
英文同义词:
4-(cis-1-Acetyl-4-((4-chlorophenyl)amino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)benzoic acid;I-BET726; I-BET 726;CS-1736;4-((2S,4R)-1-acetyl-4-(4-chlorophenylamino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)benzoic acid;GSK1324726A;4-[(2S,4R)-1-Acetyl-4-[(4-chlorophenyl)amino]-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl]benzoic acid;GSK1324726A (I-BET726);4-[(2S,4R)-1-Acetyl-4-[(4-chlorophenyl)amino]-1,2,3,4-tetrahydro-2-methyl-6-quinolinyl]benzoic acid
相关类别:
细胞生物学试剂;抑制剂;小分子抑制剂，天然产物;Inhibitors
沸点
707.3±60.0 °C(Predicted)
密度
1.304±0.06 g/cm3(Predicted)
酸度系数(pKa)
4.20±0.10(Predicted)
生物活性
GSK1324726A（I-BET726）是BET家族蛋白的高选择性抑制剂，对BRD2, BRD3, 和BRD4的IC50分别为41 nM, 31 nM,和22 nM。
体外研究
In neuroblastoma cell lines, GSK1324726A inhibits cell growth and induces cytotoxicity. GSK1324726A also modulates expression of genes involved in apoptosis, signaling, and MYC-family pathways, including the direct suppression of BCL2 and MYCN.
体内研究
In the mouse SK–N-AS and CHP-212 models, GSK1324726A (15 mg/kg p.o.) results in tumor growth inhibition and down-regulation MYCN and BCL2 expression. In a mouse septic shock model, GSK1324726A (10 mg/kg i.v.) shows potent anti-inflammatory effects, and prevents death of diseased animals.
