Biochem/physiol Actions
ATP-competitive, potent and selective inhibitor against cyclin-dependent kinase Cdk5 both in vitro and in vivo.
CP-681301 is a potent, ATP-competitive cyclin-dependent kinase Cdk5 inhibitor (Ki = 13.7 nM; 2.8-/40-fold selectivity over Cdk2/GSK-3β) that blocks Cdk5 substrates phosphorylation in cultures (tau pS235 IC50 = 513 nM in CHO p25/CDK5/tau transfectants; IC50 ~500 nM against 48-h 10 µM oligomeric Aβ42-stimulated APP pT668 in murine embryonic neurons) and reverses the upregulated tau pS235 level in Cdk5 activator p25-overexpressing transgenic neonatal mice in vivo (5.8 mg/kg s.c.; 6 hrs). CP-681301 selectively inhibits Cdk5-dependent proliferation of human medullary thyroid carcinoma (MTC), but not normal human fibroblasts in cultures (5 µM, 48 hrs).
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
| SMILES string | O=C(CC1=CC=C(C=C1)N(C)C)NC2=CC(C3CCC3)=NN2 |
| InChI | 1S/C17H22N4O/c1-21(2)14-8-6-12(7-9-14)10-17(22)18-16-11-15(19-20-16)13-4-3-5-13/h6-9,11,13H,3-5,10H2,1-2H3,(H2,18,19,20,22) |
| InChI key | PGTNTDKBRSQDNM-UHFFFAOYSA-N |
