CDK2-IN-31 is a potent inhibitor of the CCNE1:CDK2 complex, exhibiting an IC50 of 0.13 μM. It binds to a unique allosteric pocket at the interface of CCNE1 and CDK2, leading to significant structural changes in the CDK2 A-loop that disrupt its active conformation and hinder substrate binding. This compound effectively inhibits the phosphorylation of retinoblastoma protein 1 (RB1) in CCNE1-dependent ovarian cancer cells and disrupts the coenrichment of protein PRC1 with CCNE1-N112C:CDK2 complexes. CDK2-IN-31 is valuable for research investigating ovarian cancer mechanisms and potential therapeutic targets.
CDK2-IN-31 is a potent inhibitor of the CCNE1:CDK2 complex, exhibiting an IC50 of 0.13 μM. It binds to a unique allosteric pocket at the interface of CCNE1 and CDK2, leading to significant structural changes in the CDK2 A-loop that disrupt its active conformation and hinder substrate binding. This compound effectively inhibits the phosphorylation of retinoblastoma protein 1 (RB1) in CCNE1-dependent ovarian cancer cells and disrupts the coenrichment of protein PRC1 with CCNE1-N112C:CDK2 complexes. CDK2-IN-31 is valuable for research investigating ovarian cancer mechanisms and potential therapeutic targets.
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