ABC1183 是一种具有口服活性的选择性GSK3和CDK9双重抑制剂。ABC1183 作用于 GSK3β, GSK3α 和 CDK9/cyclin T1 的IC50值分别是 657 nM、327 nM、321 nM。ABC1183 具有抗炎作用，抗肿瘤活性。
| 生物活性 | ABC1183 is an orally active selective dualGSK3andCDK9inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with theIC50values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities[1].
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| IC50& Target[1] | CDK9- Cyclin T1 321 nM (IC50) | GSK-3α 327 nM (IC50) | GSK-3β 657 nM (IC50) |
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体外研究
(In Vitro) | ABC1183 (3 μM, 24 h) can block cell cycle progression and thus affect cell proliferation[1].
Cell Cycle Analysis[1] | Cell 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. |
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体内研究
(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[1].
| Animal Model: | Male C57BL/6 mice with melanoma B16[1] | | 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 infectedcrohn’sdisease[1] | | 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[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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