CDK Inhibitor

BS-181 dihydrochloride is a potent and selective CDK7 inhibitor (IC₅₀=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC₅₀ values of 880 nM, 3000 nM and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel of cancer cells growth (IC₅₀=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 dihydrochloride has the potential for the research of cancer therapy.

rel-AZ5576 is a selective CDK9 inhibitor with the activity of downregulating Mcl-1 and MYC mRNA transcription and protein expression in diffuse large B-cell lymphoma by inhibiting CDK9, promoting MYC protein turnover, reducing MYC phosphorylation on the stable Ser62 residue and downregulating MYC transcriptional targets, inhibiting the growth of diffuse large B-cell lymphoma cell lines in vitro and in vivo and independent of the cell origin.

CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor with K_is of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a K_i of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma.

CDK9-IN-9 (example 2) is a potent and selective CDK9 inhibitor with an IC₅₀ of 1.8 nM. CDK9-IN-9 inhibits CDK2 with an IC₅₀ of 155 nM. CDK9-IN-9 has anti-cancer activity.

CDK7-IN-11 is an orally active CDK7 inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC₅₀ value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7.

CDK9-IN-29 (compound Z11) is a potent CDK9 inhibitor (IC₅₀ = 3.20 nM) with good kinase selectivity. CDK9-IN-29 inhibits cell proliferation and induces apoptosis.

Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC₅₀s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib shows antitumor activity on cisplatin-resistant cells.

Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC₅₀ values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively.

Senexin A hydrochloride is an inhibitor of CDK8/19 (IC₅₀: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A hydrochloride inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters.

Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

Amantadine (1-Adamantanamine) sulfate is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine sulfate inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine sulfate also has anti-orthopoxvirus and anticancer activity. Amantadine sulfate can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.

QR-6401 is an orally active and selective macrocyclic CDK2 inhibitor with IC₅₀ values of 0.37, 10, 22, 34 and 45 nM for CDK2/E1, CDK9/T1, CDK1/A2, CDK6/D3 and CDK4/D1, respectively. QR-6401 has potent antitumor activity in an OVCAR3 ovarian cancer xenograft model. QR-6401 has the potential to be used in the study of cancer.

CDK7-IN-30 (Compound 22) is a CDK7 inhibitor (IC₅₀ = 7.21 nM) that effectively inhibits the phosphorylation of RNA Polymerase II and CDK2. CDK7-IN-30 CDK7-IN-30 can induce cell apoptosis and has anti-cancer activity and can be used in cancer research.

CDK2-IN-41 (Compound 7a) is a CDK2 inhibitor that exerts anticancer activity by binding to CDK2, thereby inhibiting the cell cycle, inducing cytotoxicity, promoting ROS production, and triggering Apoptosis. CDK2-IN-41 exhibits an IC₅₀ of 10 µM against acute myeloid leukemia (AML) HL-60 cells. It holds potential for research in AML-related cancer therapy.

A-1592668 is a selective CDK9 inhibitor. A-1592668 induces Apoptosis. A-1592668 plus Venetoclax (HY-15531) co-treatment inhibits the growth of Jeko-1 tumors.

CDK7-IN-6 is a potent and selective cyclin-dependent kinase (CDK7) inhibitor (IC₅₀≤100 nM), extracted from patent WO2019197549 A1, compound 210. CDK7-IN-6 is > 200-fold selective for CDK7 over CDK1, CDK2, and CDK5. CDK7-IN-6 can be used for the research of cancer.

CDK-IN-13 (compound 32E) is a potent and selective inhibitor of CDK12/cyclinK with an IC₅₀ of 3 nM. CDK-IN-13 inhibits the growth of the HER2-positive breast cancer cell lines.

CDK2/4-IN-1 (compound B-4a) is a CDK2/4 inhibitor and a tubulin polymerization inhibitor. CDK2/4-IN-1 can be used in cancer research.

CDK2/4 ligand 1 is a ligand for target protein for PROTACs, which targets CDK2/4. CDK2/4 ligand 1 can be used for synthesis of PROTAC CDK2/4 Degrader-1 (HY-179688).