3081311-94-3
Chemical Structure
LL-K12-18
- CAS No.: 3081311-94-3
- Formula:C25H32Cl2N10O
- Molecular Weight:559.49
InChIKey: OTSBHVNFWKVPMY-UHFFFAOYSA-N
SMILES: CCN1C=NC2=C1N=C(N(CC3)CCN3C(CN(CC)CC)=O)N=C2NCC4=NC5=CC(Cl)=C(C=C5N4)Cl
Biological Activity:
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, γ-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].
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LL-K12-18 | 98.42% | 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, γ-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. |
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- [1]. Zhang Z, Li Y, Yang J, et al. Dual-site molecular glues for enhancing protein-protein interactions of the CDK12-DDB1 complex[J]. Nature Communications, 2024, 15(1): 6477.
- [2]. Lin S, Yang C G, Luo C, et al. Recent Advances in Dynamic Biomacromolecular Modifications and Chemical Interventions: Perspective from a Chinese Chemical Biology Consortium[J]. CCS Chemistry, 2025, 7(10): 2912-2949.
Keywords
