LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC 50 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 .
Products | Products > Disease Areas > Cancer | Products > Disease Areas > Breast Cancer | Products > Disease Areas > Triple-Negative Breast Cancer | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Cell Cycle/DNA Damage | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > PI3K/Akt/mTOR | Products > Signaling Pathways > Epigenetics | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > RAD51 | Products > Signaling Pathways > ATM/ATR | Products > Signaling Pathways > PARP | Products > Signaling Pathways > DNA/RNA Synthesis | Products > Signaling Pathways > Molecular Glues | Products > Signaling Pathways > CDK
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