LL-K8-22 is a potent, selective and durable CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research.
LL-K8-22 (0-10 μM, 24 h) degrades the CDK8-cyclin C complex in a dose-dependent manner[1]. LL-K8-22 (0-20 μM, 4 days) suppresses tumor cell proliferation[1].LL-K8-22 (0-8 μM, 24 h) inhibits CDK8-cyclin C downstream signaling[1]. LL-K8-22 significantly downregulated EAPP (E2F family binding protein)[1].LL-K8-22 dose not affect CDK8 and CCNC mRNA levels[1].
References:
[1]. Wang M, et al. Discovery of LL-K8-22: A Selective, Durable, and Small-Molecule Degrader of the CDK8-Cyclin C Complex. J Med Chem. 2023 Apr 13;66(7):4932-4951.
















