LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, gamma-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer[1][2].
Molecular Weight:
559.49
Purity:
98.42
CAS Number:
[3081311-94-3]
Formula:
C25H32Cl2N10O
Target:
Apoptosis,ATM/ATR,CDK,Molecular Glues,PARP,RAD51
Application Notes:
MCE Product type: Reference compound
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