THAL-SNS-032

THAL-SNS-032 is a selective, small-molecule proteolysis-targeting chimera (PROTAC) designed to induce the degradation of Cyclin-Dependent Kinase 9 (CDK9). It is a chimeric molecule consisting of the CDK inhibitor SNS-032 conjugated to a thalidomide derivative, which serves as a ligand for the Cereblon (CRBN) E3 ubiquitin ligase. By recruiting CRBN to CDK9, THAL-SNS-032 facilitates the ubiquitination and subsequent proteasomal degradation of the kinase. Depletion of CDK9 leads to the inhibition of RNA polymerase II phosphorylation, resulting in the downregulation of short-lived oncogenic proteins such as Mcl-1, c-Myc, and Mdm2, and the stabilization of p53. This mechanism effectively inhibits tumor cell proliferation and induces apoptosis. THAL-SNS-032 has been primarily investigated as a research tool and preclinical candidate for the treatment of multiple myeloma and other hematologic malignancies.

Other names

Thal-SNS-032Thal-SNS032Thal-SNS 032