产品
编 号:F018706
分子式:C18H14N4OS
分子量:334.39
产品类型
结构图
CAS No: 1042735-18-1
联系客服
产品详情
生物活性:
ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities.
体内研究:
ABC1183 (oral gavage, 5 or 50 mg/kg) inhibits tumor proliferation through negative regulation of cell growth and pro-inflammatory signalling in male C57BL/6 mice.Animal Model:Male C57BL/6 mice with melanoma B16
Dosage:5 mg/kg
Administration:Oral gavage; 5 times per week; 22 days
Result:Reduced tumor size and no observed toxicity.Decreased the expression levels of GSK3 α /β, pSer21/9 and GS pSer641 but no change of total GS expression.
Animal Model:Male C57BL/6 mice infected crohn’s disease
Dosage:50 mg/kg
Administration:Oral gavage; everyday; 3 days
Result:Reduced TNF-α by 65%, IL-6 by 30% and IL-1β by 45%.
Animal Model:Male C57BL/6 mice with ulcerative colitis
Dosage:50 mg/kg
Administration:Oral gavage; once daily; 6 days
Result:Increased the expression of the anti-inflammatory factor IL-10, while decreasing the pro-inflammatory factor IL-6.
体外研究:
ABC1183 (3 μM, 24 h) can block cell cycle progression and thus affect cell proliferation.