2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. CDK
  5. CDK13 Isoform
  6. CDK13 Inhibitor

CDK13 Inhibitor

CDK13 Inhibitors (10):

Cat. No. Product Name Effect Purity
  • HY-80013
    THZ1
    		Inhibitor 99.84%
    THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
  • HY-103618
    THZ531
    		Inhibitor 99.86%
    THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively.
  • HY-130250
    SR-4835
    		Inhibitor 99.73%
    SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death.
  • HY-80013A
    THZ1 Hydrochloride
    		Inhibitor 99.06%
    THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
  • HY-173042
    CDK12/13-IN-2
    		Inhibitor
    CDK12/13-IN-2 (Compound 24) is a covalent inhibitor of CDK12/13, with IC50 values of 15.5 nM and 12.2 nM for CDK12 and CDK13, respectively. CDK12/13-IN-2 can inhibit the proliferation of breast cancer cells and can be used in the research of triple-negative breast cancer.
  • HY-145072
    BSJ-01-175
    		Inhibitor 99.45%
    BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells.
  • HY-142696
    CDK6/PIM1-IN-1
    		Inhibitor
    CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity.
  • HY-173059
    CDK12/13-IN-3
    		Inhibitor
    CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6%.
  • HY-158170
    CDK7-IN-28
    		Inhibitor
    CDK7-IN-28 (CDK7-1276) is a potent CDK7 inhibitor(IC50＜5 nM). CDK7-IN-28 can inhibit proliferation of MDA-MB-468 cell line by blocking cell cycle and inhibiting DNA replication.
  • HY-150641
    CDK-IN-9
    		Inhibitor
    CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II.