For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I041373 |
| Synonyms | 1-[4-[3-(1-adamantyl)propyl]piperazin-1-yl]-2-[4-(4-isoquinolin-4-ylphenyl)pyrazol-1-yl]ethanone |
| Molecular Formula | C37H43N5O |
| Purity | ≥95% |
| InChI | InChI=1S/C37H43N5O/c43-36(41-14-12-40(13-15-41)11-3-10-37-19-27-16-28(20-37)18-29(17-27)21-37)26-42-25-33(23-39-42)30-6-8-31(9-7-30)35-24-38-22-32-4-1-2-5-34(32)35/h1-2,4-9,22-25,27-29H,3,10-21,26H2 |
| InChIKey | WXQLBECTYSLDGB-UHFFFAOYSA-N |
| SMILES | C1CN(CCN1CCCC23CC4CC(C2)CC(C4)C3)C(=O)CN5C=C(C=N5)C6=CC=C(C=C6)C7=CN=CC8=CC=CC=C87 |
| 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. |
