ABC1183

ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC 50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities

In Vitro

ABC1183 (3 μM, 24 h) can block cell cycle progression and thus affect cell proliferation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: LNCaP human prostate cancer cells Concentration: 3 μM Incubation Time: 24 hours Result: Significantly reduced cells in the G1 and S phases and increased cells in the G2/M and sub-G1 cycle phases.

In Vivo

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.

IC50& Target:CDK9- Cyclin T1 321 nM (IC 50 ) GSK-3α 327 nM (IC 50 ) GSK-3β 657 nM (IC 50 )