cyclind1

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.

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].

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.

LDC000067 (LDC067) is a highly specific and selective CDK9 inhibitor with an IC50 value of 44±10 nM.

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

AT7519 is a CDK1 2 4 6 9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.

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.

Milciclib (PHA-848125) (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2.

FIDAS-5 is an orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. It can effectively compete with S-adenosylmethionine for MAT2A binding and has anticancer effects.

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.

PU02 (6-[(1-Naphthalenylmethyl)thio]-9H-purine) is a potent and selective antagonist of 5-HT3 receptor.

FIDAS-3, a stilbene derivative and potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A), exhibits anticancer activities by effectively competing with S-adenosylmethionine (SAM) for MAT2A binding.

PNU-292137 is an inhibitor of CDK2 cyclin A with the activity of antitumor.

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.

Purvalanol A (NG-60) is an effective and cell-permeable CDK inhibitor with IC50 of 70 4 35 850 nM for cdk2-cyclin A B E, and cdk4-cyclin D1, respectively.

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

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

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.

Indirubin-5-sulfonate shows inhibitory activity against GSK-3β. Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1 cyclin B, CDK2 cyclin A, CDK2 cyclin E, CDK4 cyclin D1,

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.

CA224 (Compound 1), an orally active and selective Cdk4–cyclin D1 inhibitor, demonstrates an IC50 of 6.2 µM. It induces cell apoptosis and exhibits antitumor activity [1].

CDK4 6-IN-9 (compound 10) is a selective inhibitor of CDK4 6, demonstrating activity on CDK6 cyclin D1 (IC50: 905 nM), and holds potential research value in multiple myeloma (MM).

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

CDK6 PIM1-IN-1 is a balanced, potent dual inhibitor of CDK6 (IC50: 39 nM) and PIM1 (IC50: 88 nM), also showing inhibitory activity on CDK4 (IC50: 3.6 nM). It significantly inhibits the proliferation of acute myeloid leukemia (AML) cells, arrests the cell cycle in G1 phase, induces cell apoptosis, and demonstrates anti-AML activity.