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.