推荐产品
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
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
生化/生理作用
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).
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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)
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 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)
Interplay between cyclin-dependent kinase 5 and glycogen synthase kinase 3 beta mediated by neuregulin signaling leads to differential effects on tau phosphorylation and amyloid precursor protein processing
Yi Wen
The Journal of Neuroscience, 28, 2624-2632 (2008)
Transcriptional regulation of beta-secretase by p25/cdk5 leads to enhanced amyloidogenic processing
Yi Wen
Neuron, 57, 680-690 (2008)
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