Skip to Content
Merck
CN

SML3512

CP-681301

≥98% (HPLC)

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

Sign In to View Organizational & Contract Pricing.

Select a Size

About This Item

Empirical Formula (Hill Notation):
C17H22N4O
CAS Number:
865317-32-4
Molecular Weight:
298.38
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

View All Documentation
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist

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

SMILES string

O=C(CC1=CC=C(C=C1)N(C)C)NC2=CC(C3CCC3)=NN2

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Quality Level

100

Related Categories

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).

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

新产品
This item has

Choose from one of the most recent versions:

Certificates of Analysis (COA)

Lot/Batch Number
0000220408
0000220409
0000220409
0000220408
0000206411

Don't see the Right Version?

If you require a particular version, you can look up a specific certificate by the Lot or Batch number.

Search for a COA

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

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)
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)
View All Related Papers

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service