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CDK5-IN-4 (compound 4) is a potent multikinase type-II inhibitor targeting CDK5, with an IC50 of 9.8 μM. CDK5-IN-4 also inhibits GSK-3α, GSK-3β, CDK9, and CDK2, with IC50 values of 0.98, 4.00, 1.76, and 6.24 μM, respectively. CDK5-IN-4 can be used for glioblastoma research[1]. | [IC 50]
GSK-3α: 0.98 ± 0.0 μM (IC50); GSK-3β: 4.00 ± 1.3 μM (IC50); CDK9: 1.76 ± 0.3 μM (IC50); CDK2: 6.24 ± 2.8 μM (IC50); CDK5: 9.8 ± 2.29 μM (IC50) | [References]
[1] Khan ZR, et al. Discovery of Potent Multikinase Type-II Inhibitors Targeting CDK5 in the DFG-out Inactive State with Promising Potential against Glioblastoma. J Med Chem. 2024 Apr 30. DOI:10.1021/acs.jmedchem.4c00373 |
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