CDK Inhibitor

AT7519 (Hydrochloride) (Standard) is the analytical standard of AT7519 (Hydrochloride). This product is intended for research and analytical applications. AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.

Olomoucine II is a potent CDK inhibitor with IC₅₀ values of 0.06, 0.1, 0.45, 7.6, 19.8 µM for CDK9/cyclin T, CDK2/cyclin E, CDK7/cyclin H, CDK1/cyclin B, CDK4/cyclin D1, respectively. Olomoucine II shows antiproliferative activity.

(S)-(-)-O-Demethylbuchenavianine (Compound (S)-(−)-1) is a flavonoidal alkaloids. (S)-(-)-O-Demethylbuchenavianine is a potent CDK inhibitor, with IC₅₀ values of 0.03 and 0.05 μM for CDK1 and CDK5, respectively.

(R)-(+)-O-Demethylbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK). (R)-(+)-O-Demethylbuchenavianine inhibits CDK1, CDK5, glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), with IC₅₀s of 1.1, 0.95, >10, >10 and >10 μM, respectively.

1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC (PC(18:0/22:4)) is an inhibitor of cyclin-dependent kinases (CDKs). 1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC induces apoptosis and inhibits the growth of various cancer cell lines.

Ribociclib succinate (Standard) is the analytical standard of Ribociclib succinate. This product is intended for research and analytical applications. Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC₅₀ of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity.

Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib dihydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.

Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.

CDK1-IN-5 (10h) is a selective CDK1 inhibitor with IC₅₀s of 42.19, 188.71 and 354.15 nM for CDK1, CDK2 and CDK5, respectively. CDK1-IN-5 inhibits growth of cancer cells by affecting cell cycle. CDK1-IN-5 can be used for the research of cancer.

Cimpuciclib is a selective CDK4 inhibitor (IC₅₀: 0.49 nM) that has anti-tumor activity.

Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

CDK1-IN-3 (8g) is a selective CDK1 inhibitor with IC₅₀s of 36.8, 305.17 and 369.37 nM for CDK1, CDK2 and CDK5, respectively. CDK1-IN-3 inhibits the growth of cancer cells by affecting cell cycle. CDK1-IN-3 can be used for the research of cancer.

HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC₅₀ values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity.

XL495 is an potent, selective and orally active PKMYT1 inhibitor. XL495 inhibits CDK1 Thr14 phosphorylation and induces KAP1 Ser824 phosphorylation in xenograft tumors. XL495 reduces tumor growth in colorectal and breast cancer xenograft models, and achieves tumor regression with DNA-damaging agents in colorectal cancer xenograft models. XL495 can be used for the research of cancer, such as breast cancer and colorectal cancer.

OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC₅₀ of 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a K_d of 40 nM.

ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC₅₀ values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC₅₀=19.023 μM) and BChE (IC₅₀=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase.

Tibremciclib is a CDK4 inhibitor with antineoplastic activity.

CDK7-IN-2 hydrochloride hydrate (Example 6) is a potent and selective CDK7 inhibitor. CDK7-IN-2 has potent anti-cancer activity.

Fovinaciclib is an orally active CDK (CDK4/6) inhibitor with antitumor activity.