All Photos(1)
Synonym(s):
CP 681301, CP681301, N-(3-Cyclobutyl-1H-pyrazol-5-yl)-2-(4-(dimethylamino)phenyl)acetamide, N-(5-Cyclobutyl-1H-pyrazol-3-yl)-2-(4-dimethylaminophenyl)acetamide, N-(5-Cyclobutyl-2H-pyrazol-3-yl)-2-(4-dimethylaminophenyl)acetamide
Empirical Formula (Hill Notation):
C17H22N4O
Recommended Products
Quality Level
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
Biochem/physiol Actions
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).
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Inhibition of Cdk5 rejuvenates inhibitory circuits and restores experience-dependent plasticity in adult visual cortex
Li Y, Wang L, Zhang X, Huang M, Li S, Wang X, Chen L, Jiang B, Yang Y
Neuropharmacology, 128, 207-220 (2018)
Cdk5 Modulates Long-Term Synaptic Plasticity and Motor Learning in Dorsolateral Striatum
Hernandez A, Tan C, Mettlach G, Pozo K, Plattner F, Bibb JA
Scientific Reports, 6, 29812-29812 (2016)
Regulation of ERK Kinase by MEK1 Kinase Inhibition in the Brain
Tassin TC, Benavides DR, Plattner F, Nishi A, Bibb JA
The Journal of Biological Chemistry, 290, 16319-16329 (2015)
Cdk5 protein inhibition and A?42 increase BACE1 protein level in primary neurons by a post-transcriptional mechanism: implications of CDK5 as a therapeutic target for Alzheimer disease
Katherine R Sadleir
The Journal of Biological Chemistry, 287, 7224-7235 (2012)
Neurodegenerative disorders and their treatment
Eric Karran, Alan M Palmer
Drug News and Perspectives, 20, 407-412 (2007)
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