cdk-9-in-1

CDK9-IN-1 is a selective and potent CDK9 inhibitor with antiviral activity used in the study of PRRSV infections.

CDK9-IN-10 is a potent inhibitor of CDK9 and serves as the ligand for the PROTAC CDK9 degrader-2.

CDK9-IN-15 is a potent small molecule CDK9 inhibitor, which can block the phosphorylation of positive transcription elongation factor b (P-TEFb) on the C-terminal region of RNA Poly-II by degradation and inhibition of CDK9, inhibit transcription, and rapidly reduce the level of intracellular mRNA, thereby causing apoptosis of tumor cells.

CDK9-IN-11 is a potent CDK9 inhibitor and serves as the ligand for the PROTAC CDK9 Degrader-1 [1].

CDK9-IN-12 is a highly selective CDK9 inhibitor, which is commonly used in leukemia research to regulate oncogene expression, inhibit oncogenic proliferation, and induce apoptosis by targeting CDK9-dependent transcription processes.

CDK9-IN-14 is a potent, high and low selective CDK9 inhibitor (IC50: 6.92 nM). CDK9-IN-14 is a strong inhibitor of MV-4-11 cells and in vivo tumour models with low toxicity and few side effects.

EGFR/HER2/CDK9-IN-1 (Compound 4) is a potent inhibitor of EGFR, HER2, and CDK9, with IC50 values of 90.17 nM, 131.39 nM, and 67.04 nM, respectively, and exhibits significant anti-tumor effects.

CDK9-IN-13 is a potent and selective CDK inhibitor (IC50<3 nM). CDK9-IN-13 has a very short half-life in rodents.

CDK9-IN-18, a potent inhibitor of CDK9, blocks its phosphorylation, exhibits good anticancer activity, induces apoptosis, and has low cellular activity.

CDK9-IN-19 is a selective and potent CDK9 inhibitor (IC50: 2.0 nM). CDK9-IN-19 exhibits good anti-proliferative activity in cancer cells, moderate pharmacokinetic properties and low hERG inhibition. CDK9-IN-19 significantly inhibited tumor growth in the MV4-11 xenograft mouse model. CDK9-IN-19 can be used in studies of acute myeloid leukemia (AML).

A09-003 is a novel cell cycle protein-dependent kinase-9 CDK-9 inhibitor.A09-003 inhibits the proliferation of a variety of leukemia cell lines and inhibits the increase of leukemia sequence-1 protein in myeloid cells.A09-003 also induces apoptosis, decreases RNA polymerase II activity, and decreases Mcl-1 expression.

CKD-712 is a nuclear factor NF-kappa B inhibitor. CKD-712 suppressed MMP-9, but not MMP-2 and other NF-κB-regulated proteins involved in cancer metastasis such as VEGF. CKD-712 induced cell cycle arrest at G2M phase by suppressing cyclin A, cyclin B and C

CDK6/9-IN-1 (compound 66) is a potent, orally administered dual inhibitor of CDK6 and CDK9, with IC50 values of 40.5 nM and 39.5 nM, respectively.

CDK7/9-IN-1 is a specific inhibitor of cyclin-dependent kinases 7/9 (CDK7/9), targeting CDK7 with IC50 values of 0.0656 μM without pre-incubation and 0.00574 μM after 3 hours pre-incubation, and displaying inhibitory activity against CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation, making it valuable for cancer research.

CDK7-IN-16 (Compound 9) is a potent inhibitor of CDK 7 (IC50: 1-10 nM). CDK7-IN-16 can be used in research against cancer, particularly cancers with transcriptional abnormalities.

Ibulocydine is a potent CDK inhibitor. Ibulocydine has high activity against Cdk7/cyclin H/Mat1 and Cdk9/cyclin T. Ibulocydine inhibited the growth of HCC cells more effectively than other Cdk inhibitors, including olomoucine and roscovitine, whereas ibulocydine as well as the other Cdk inhibitors and BMK-Y101 minimally influenced the growth of normal hepatocyte cells. Ibulocydine induced apoptosis in HCC cells, most likely by inhibiting Cdk7 and Cdk9. In vitro treatment of HCC cells with ibulocydine rapidly blocked phosphorylation of the carboxyl-terminal domain (CTD) of the large subunit of RNA polymerase II, a process mediated by Cdk7/9. Anti-apoptotic gene products such as Mcl-1, survivin, and X-linked IAP (XIAP) are crucial for the survival of many cell types, including HCC. Following the inhibition of RNA polymerase II phosphorylation, ibulocydine caused rapid down-regulation of Mcl-1, survivin, and XIAP, thus inducing apoptosis. Furthermore, ibulocydine effectively ind......

CDK4/6-IN-14 is a potent, highly selective inhibitor of Cyclin-Dependent Kinases 4 and 6 (CDK4/6), with inhibition concentrations (IC50s) of 10 nM and 16 nM, respectively. It shows over 60-fold selectivity for CDK4/6 compared to CDKs 1, 2, 7, and 9, and exhibits significant selectivity against 205 other kinases.

CDK2-IN-26, also known as compound 9, effectively inhibits CDK 2 [1].