HQ461 Hydrobromide，5MG，SML2994-5MG，Sigma

Biochem/physiol Actions

CDK12 kinase domain-targeting molecular glue that impairs CDK12/13 downstream signaling by inducing cyclin K (CycK) ubiquitination and degradation.
HQ461 is a CDK12 kinase domain-targeting molecular glue that promotes CDK12 interaction with DDB, resulting in DDB1-CUL4-RBX1 E3 ubiquitin ligase complex-mediated CDK12-interacting protein cyclin K (CycK) polyubiquitination and degradation (1-10 μM; A549). HQ461 treatment impairs A549 cellular CDK12 and CDK13 downstream signaling events, including RNA pol II C-terminal domain (CTD) Ser2 phosphorylation (1-10 μM) and DNA damage response genes expression (10 μM, 16 hrs).