cdk5/p25

PHA-793887 has been used in trials studying the treatment of Advanced Metastatic Solid Tumors.

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.

MeBIO is an agonist of aryl hydrocarbon receptor, with IC50 of 44 and 55 μM for GSK-3 and CDK1 CyclinB, respectively. MeBIO does not affect GSK-3β.

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.

Indirubin-3'-monoxime (Indirubin-3'-oxime) is a potent inhibitor of GSK3β (IC50: 22 nM) and also inhibits CDKs ( (IC50s: 100 180 250 nM for Cdk5 p35, Cdk1 cyclin B, Cdk2 cyclin E).

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

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).

DSS30 is a P25 CDK5 inhibitor.DSS30 acts by inhibiting the phosphorylation of amyloid precursor protein cleaving enzyme 1 (BACEl), which reduces the secretion of β-amyloid (Aβ).DSS30 can be used for the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease.

Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).

Abemaciclib (LY2835219) is a dual inhibitor of CDK4 6 (IC50=2 10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

KenPaullone (9-Bromopaullone), a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through increased and prolonged transcription of foxp3 gene by enhancing TGFβ-Smad3 signaling pathway.

Aloisine A is a potent and selective CDK/GSK-3 inhibitor. IC50 data of Aloisine A: Cdk1/cyclin B (IC50: 150nM), Cdk2/cyclin A (IC50: 120nM), Cdk2/cyclin E (IC50: 400nM), Cdk5/p25 (IC50: 200nM), Cdk5/p35 (IC50: 160nM), GSK-3α (IC50: 500nM), GSK-3β (IC50: 6

LDN-193665 is a potent inhibitor of tau kinase. It acts by targeting CDK5/p25 and GSK3β.

NU6140 is a selective inhibitor of CDK2-cyclin A (IC50, 0.41 μM). It shows 10- to 36-fold selectivity over other CDKs. NU6140 also effectively inhibits Aurora A and Aurora B (IC50s: 67 and 35 nM, respectively). It also enhances the apoptotic effect and has anti-cancer activity.

CGP60474 is an inhibitor of VEGFR-2 (IC50 = 84 nM) and an inhibitor of ATP-competitive PKC. CGP60474 is also a highly potent anti-endotoxemic agent and inhibits cyclin-dependent kinase (CDK) potently.

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.

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.

CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor targeting CDK5 p25 (IC50: 0.2 nM) and CDK2 CycA (IC50: 23 nM).

1-Azakenpaullone (azakenpaullone) is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1 cyclin B and CDK5 p25.

CDK-IN-9 (compound 24) is a potent inhibitor of CDK and acts on CDK2 E (IC50: 4 nM). It functions as a molecular gel that induces interaction between CDK12 and DDB1, and can dephosphorylate retinoblastoma protein and RNA polymerase II, thereby inducing apoptosis.

(E Z) - BIO-acetoxime is effective and selective GSK-3 α β Inhibitors. For GSK-3 α β, CDK5 p25, CDK2 cyclin A and CDK1 cyclin B, IC50 are 10nM, 2.4 μM, 4.3 μ M, 63 μ M, respectively.

cdk CK1 inhibitor,potent and ATP-competitive