cdk6/cyclind1

FN-1501 is a potent FLT3 and CDK inhibitor (IC50s: 2.47, 0.85, 1.96, and 0.28 nM for CDK2 cyclin A, CDK4 cyclin D1, CDK6 cyclin D1 and FLT3, respectively). FN-1501 also has anticancer activity.

GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4/6, exhibiting IC50 values of 1.5 μM for CDK4/cyclin D1, 5.6 μM for CDK6/cyclin D1, and 25 μM for Cdk5/p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

Palbociclib (PD 0332991) is a CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11/16 nM) and is orally active. Palbociclib has anti-tumorigenic activity and has investigational potential for use in ER-positive and HER2-negative breast cancer.

Palbociclib monohydrochloride (PD 0332991 hydrochloride) is a selective inhibitor of CDK4/6 (IC50s: 11/16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.

Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 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.

BS-181 is a highly selective CDK7 inhibitor (IC50: 21 nM); >40-fold selective for CDK7 than CDK1 2 4 5 6 9.

Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM) that represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma and effectively blocks CDK9, the transcriptional regulator of MCL-1.

Lerociclib (G1T38) is a selective and highly potent CDK4/6 inhibitor with anticancer and antitumor activity, inhibits CDK4/CyclinD1 and CDK6/CyclinD3, and inhibits tumor growth in an animal model of endocrine-resistant breast cancer. Due to the poor solubility, for animal studies, the salt form T11345L is recommended.

Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective CDK4/CDK6 inhibitor, with IC50 values of 2 nM for CDK6/CyclinD3 and 1 nM for CDK4/CyclinD1.

Palbociclib-d8 (PD 0332991 D8) is the 2H-labeled form of Palbociclib. Palbociclib is an orally active CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11/16 nM). Palbociclib has anti-tumor activity and is used in research for estrogen receptor-positive and HER2-negative breast cancer.

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

Trilaciclib hydrochloride (G1T28 hydrochloride) is an inhibitor of CDK4 6 (IC50s: 1 nM and 4 nM for CDK4 and CDK6).

Voruciclib hydrochloride is an orally active and selective CDK inhibitor with a Ki range of 0.626 nM to 9.1 nM.

AT7519 Hydrochloride (AT7519 HCl) is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9.

AT7519 is a kinase inhibitor (IC50: 0.19, 0.044, 0.51, 0.067, 0.66 and 0.018 μM for CDK1/cyclinB, CDK2/CyclinA, CDK2/Cyclin E, CDk4/CyclinD1, CDK6/Cyclin D3, CDk5/p35).

AZD-5438 is an effective inhibitor of CDK, for CDK1(IC50=16 nM), CDK2(IC50=6 nM), CDK9(IC50=20 nM).

RGB-286147 is a potent, selective, ATP-competitive Cdks inhibitor.

BSJ-03-204 is a selective Cdk4/6 degrader.

Selective Cdk4 degrader. Degrades Cdk4 in Molt-4 cells, with no effect on Cdk6 levels. Displays cereblon-dependent degradation. Jiang et al (2019) Development of dual and selective degraders of cyclin-dependent kinases 4 and 6. Angew.Chem.Int.Ed.Engl. 58 6321 PMID:30802347

SR-3029 is a highly potent and specific inhibitor of CK1δ/CK1ε.

MC180295 ((rel)-MC180295) is a novel, potent, and highly selective CDK9 inhibitor with an IC50 of 5 nM, demonstrating over 22-fold selectivity compared to other CDKs.

JNJ-7706621 is a potent aurora kinase inhibitor that also inhibits CDK1 and CDK2.

BS-181 hydrochloride (BS-181 HCl) is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.