Bioactivity | 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[1]. |
Invitro | LL-K8-22 (0-10 μM, 24 h) 以剂量依赖性方式降解 CDK8-cyclin C 复合物[1]。LL-K8-22 (0-20 μM,4 天) 抑制肿瘤细胞增殖[1]。LL-K8-22 (0-8 μM, 24 h) 抑制 CDK8-cyclin C 下游信号[1]。LL-K8-22 显著下调 EAPP (E2F 家族结合蛋白)[1]。LL-K8-22 不影响 CDK8 和 CCNC mRNA 水平[1]。 Western Blot Analysis[1] Cell Line: |
Name | LL-K8-22 |
Formula | C37H43N5O |
Molar Mass | 573.77 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |