cdk7/9 in 1

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.

JAK1/CDK7-IN-1 (compound 11) is a JAK1/CDK7 inhibitor and cytotoxic agent. It forms a stable and tightly bound complex with JAK1, disrupts the cell cycle, induces G2/M phase arrest, and increases the proportion of cells in the G1 phase. Additionally, JAK1/CDK7-IN-1 induces apoptosis, elevates levels of caspase 1, 3, and 9, and triggers both apoptotic and necrotic cell death. This compound is applicable in research related to breast and prostate cancer.

Olomoucine II is a potent cyclin-dependent kinase inhibitor with IC50 values of 7.6, 0.1, 19.8, 0.45, and 0.06 μM for CDK1, CDK2, CDK4, CDK7, and CDK9, respectively. Olomoucine II demonstrates high selectivity over numerous other kinases while retaining measurable activity against ERK2 and ABCB1, allowing it to modulate multidrug resistance pathways. Olomoucine II suppresses proliferation across cancer cell lines regardless of p53 status and exhibits synergistic action with daunorubicin in ABCB1-expressing HCT-8 cells.Olomoucine II additionally inhibits replication of HSV-1, HSV-2, vaccinia virus, adenovirus 4, and human CMV, making Olomoucine II an important antiviral and anticancer research tool.

CDK7/9 tide is a peptide substrate for CDK7 or CDK9[1].

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......