CDK6 Inhibitor

Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib 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.

Abemaciclib (LY2835219) is a selective and BBB-permeable CDK4/6 inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

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

Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib monohydrochloride 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.

Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective and BBB-permeable CDK4/6 inhibitor with IC₅₀s of 2 nM and 10 nM for CDK4 and CDK6, respectively.

Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib isethionate 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.

Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC₅₀ of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI₅₀ values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects.

Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC₅₀ value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC₅₀ value of 79 nM.

AT7519 (AT7519M) as 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.

JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC₅₀s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively.

RRibociclib (LEE011) succinate is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK), with K_i values of 0.09 nM, 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6, respectively. PF-06873600 has potential antineoplastic activity.

AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC₅₀s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6 .

RRibociclib (LEE011) hydrochloride is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

BSJ-03-204 is a PROTAC linking a Cereblon ligand to a CDK ligand, serving as a potent and selective dual degrader of CDK4/6. BSJ-03-204 exhibits IC₅₀ values of 26.9 nM and 10.4 nM against CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 can be utilized for cancer-related research.

Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways.

Dalpiciclib (SHR-6390) is an orally active and highly selective inhibitor of CDK4 and 6 with IC₅₀ values of 12.4 nM and 9.9 nM, respectively. Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma.

KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC₅₀ of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity.

XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells.