cyclin k degrader

Cyclin K degrader 1 is a Cyclin K degrader.Cyclin K degrader 1 is a degrader converted from AT-7519.Cyclin K degrader 1 has weak degrading activity against Cyclin K but does not result in a sustained decrease in degradation affinity.Cyclin K degrader 1 is a degrader converted from AT-7519.

dCeMM3 (2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide) is a glue degrader. dCeMM3 prompts an interaction of CDK12-cyclin K with a CRL4B ligase complex, result in inducing ubiquitination and degradation of cyclin K.

NCT02, a cyclin K degrader, promotes the ubiquitination and proteasomal degradation of cyclin K (CCNK) and its complex partner CDK12, showing promise for metastatic colorectal cancer (CRC) research[1].

dCeMM4 (Compound 5) is a glue degrader that promotes cyclin K ubiquitination and degradation by facilitating the interaction between CDK12-cyclin K and a CRL4B ligase complex [1].

dCeMM2 is a glue degrader. dCeMM2 prompts an interaction of CDK12-cyclin K with a CRL4B ligase complex, leading to the ubiquitination and degradation of cyclin K.

PP-C8, a potent and selective PROTAC CDK12-Cyclin K degrader, efficiently induces degradation of CDK12 and Cyclin K, with DC50 values of 416 nM and 412 nM, respectively. This compound exhibits significant synergistic antiproliferative effects when combined with a PARP inhibitor in triple-negative breast cancer (TNBC) [1].

BSJ-5-63 is an effective degrader of CDK12, CDK7, and CDK9. It reduces the protein expression of CDK12, CDK7, CDK9, RNAPII, and Cyclin K, and also decreases the mRNA expression of BRCA1 and BRCA2. BSJ-5-63 exhibits anticancer activity and holds potential for prostate cancer research.

HQ461 is a molecular glue that promotes CDK12-DDB1 interaction, triggering cyclin K degradation, decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death.