cdk 5

Dinaciclib (SCH 727965) is a selective CDK inhibitor targeting CDK1, CDK2, CDK5, and CDK9 (IC50 = 3/1/1/4 nM). It exhibits potential antitumor activity by inhibiting the incorporation of thoracic glycan (dThd) DNA.

NVP-LCQ195 (LCQ-195) (AT9311) is a potent inhibitor of CDK1, CDK2, CDK3 and CDK5 (IC50: 1-42 nM).

Cyclin-dependent kinase 5 (Cdk5) is a serine/threonine kinase that is predominantly active in neuronal tissues. With p25 or p35, Cdk5 phosphorylates a range of proteins, including histone H1 and tau. Cdk5 Substrate acetate is a synthetic peptide (PKTPKKAKKL) corresponding to a sequence of histone H1. It is phosphorylated by Cdk5 with a Km value of 5 µM.

(R)-CR8 trihydrochloride (CR8, (R)-Isomer trihydrochloride) is a CDK1/2/5/7/9 inhibitor that acts as a molecular glue degrader with neuroprotective activity and induces apoptosis.

7-bromoindirubin-3'-oxime (7BIO) is a caspase independent nonapoptotic cell death inducer. 7BIO is an inhibitor of FLT3, DYRK1A, DYRK2, Aurora B and Aurora C kinases.

IC261 (SU-5607) is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.

CDK5-IN-3 is a selective and potent CDK5 inhibitor that inhibits CDK5/p25 and CDK2/CycA and can be used in the study of cancer.

Alsterpaullone is a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells Through Apoptosis-Inducing Effec

5-Iodo-indirubin-3'-monoxime is a potent inhibitor of GSK-3β, CDK5 P25, and CDK1 cyclin B, competing with ATP for binding to the catalytic site of the kinase (IC50s: 9, 20, and 25 nM).

dCeMM3 (2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide) is a glue degrader. dCeMM3 prompts an interaction of CDK12-cyclin K with a CRL4B ligase complex, result in inducing ubiquitination and degradation of cyclin K.

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,

(R)-CR8 ((R)-Isomer) is a potent and selective CDK inhibitor.

Roniciclib (BAY 1000394) is a potent pan-CDK inhibitor and a novel oral cytotoxic agent. Roniciclib inhibits the activity of cell-cycle CDKs CDK1, CDK2, CDK3, CDK4, and of transcriptional CDKs CDK7 and CDK9 with IC(50) values in the range between 5 and 25 nmol L.

AZD-5597 ((S)-(4-((5-Fluoro-4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl)amino)phenyl)(3-(methylamino)pyrrolidin-1-yl)methanone) is a potent imidazole pyrimidine amide CDK inhibitor.

YKL-5-124, a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for CDK7/Mat1/CycH, CDK2 and CDK9 respectively, displays biochemical and cellular selectivity for CDK7 over CDK12/13.

RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.

GSK-3 CDK5 CDK2-IN-1 is an imidazole derivative compound that inhibits cdk5, cdk2, and GSK-3.it has demonstrated applications in cancer research and the study of neurodegenerative diseases [1].

Cyclin-dependent kinase 5 (Cdk5) is a serine/threonine kinase that is predominantly active in neuronal tissues. With p25 or p35, Cdk5 phosphorylates a range of proteins, including histone H1 and tau. Cdk5 substrate is a synthetic peptide (PKTPKKAKKL) corresponding to a sequence of histone H1. It is phosphorylated by Cdk5 with a Km value of 5 μM.

Manzamine A hydrochloride is an orally active beta-carboline alkaloid that exhibits specific inhibitory effects on GSK-3β (IC50 = 10.2 μM) and CDK-5 (IC50 = 1.5 μM). Additionally, it targets vacuolar ATPases, leading to the inhibition of autophagy in pancreatic cancer cells. Manzamine A hydrochloride possesses antimalarial and anticancer properties, and also demonstrates potent activity against HSV-1[4].

CDK7-IN-5, a CDK7 inhibitor with an IC 50 value of less than 100 nM, exhibits potent anticancer properties (WO2015154022A1, Compound 104).

CDK4 6-IN-5 is a highly effective inhibitor of CDK4 and CDK6, with Ki values of 0.2 nM for CDK4 Cyclin D1 and 4.4 nM for CDK6 Cyclin D3 (WO2019207463A1, example A93).

CDK5-IN-1 is a highly potent inhibitor of CDK5, displaying an inhibitory activity of less than 10 nM. This potent compound is specifically employed in scientific investigations relating to kidney diseases.

CDK12-IN-5 is a potent CDK12 inhibitor with potential anticancer and antitumor activity, and can be used orally in the study of breast and ovarian cancer.

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.