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Medchemexpress LLC BSJ-4-116 | 2519823-34-6 | 99.9% | 837.38 | 50 MG
Supplier: Medchemexpress LLC HY13903950MG
BSJ-4-116 is a PROTAC (proteolysis-targeting chimera) designed to selectively degrade CDK12 (Cyclin-Dependent Kinase 12) with high potency, evidenced by an IC50 of 6 nM. It achieves its effect by linking ligands for Cereblon and CDK, leading to the downregulation of DNA damage response (DDR) genes through premature transcriptional termination and increased poly(adenylation). This compound exhibits significant antiproliferative capabilities, both as a standalone agent and in combination with the PARP inhibitor Olaparib. It has been shown to decrease CDK12 protein levels regardless of the cell line's mutational status and can overcome resistance due to specific CDK12 mutations.
- Highly potent and selective CDK12 degrader
- Downregulates DNA damage response genes
- Exhibits antiproliferative effects
- Can overcome resistance from specific CDK12 mutations
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