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Merck
CN

5.31167

GSK-3 Inhibitor XXIX, CHIR98014

别名:

GSK-3 Inhibitor XXIX, CHIR98014, N²-(2-(4-(2,4-Dichlorophenyl)-5-(1H-imidazol-1-yl)pyrimidin-2-ylamino)ethyl)-5-nitropyridine-2,6-diamine, N⁶-(2-((4-(2,4-Dichlorophenyl)-5-(1H-imidazol-1-yl)-2-pyrimidinyl)amino}ethyl)-3-nitro-2,6-pyridinediamine, CHIR-98014, CT-98014

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关于此项目

经验公式（希尔记法）:
C20H17Cl2N9O2
化学文摘社编号:
252935-94-7
分子量:
486.31
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD10565922
Assay:
≥95% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze
protect from light

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SMILES string

Clc1c(ccc(c1)Cl)c2nc(ncc2[n]4cncc4)NCCNc3nc(c(cc3)[N+](=O)[O-])N

InChI

1S/C20H17Cl2N9O2/c21-12-1-2-13(14(22)9-12)18-16(30-8-7-24-11-30)10-27-20(29-18)26-6-5-25-17-4-3-15(31(32)33)19(23)28-17/h1-4,7-11H,5-6H2,(H3,23,25,28)(H,26,27,29)

InChI key

MDZCSIDIPDZWKL-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 25 mg/mL

storage temp.

2-8°C

Quality Level

100

相关类别

Biochem/physiol Actions

Cell permeable: yes
Primary Target
GSK-3 α & β
Target IC50: 650 and 580 pM for GSK-3&alpha
Target Ki: 870 pM for human GSK-3&beta

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable, highly potent, ATP-competitive, reversible inhibitor of both GSK-3α and β (IC₅₀ = 650 and 580 pM, respectively).
A cell-permeable, brain permeant aminopyrimidine compound that acts as a potent, ATP-competitive and reversible inhibitor of both GSK-3α and β (IC50 = 650 and 580 pM, respectively; Ki = 870 pM for human GSK-3β) and significantly affects downstream effects of GSK-3. Displays excellent selectivity over closely related Cdc2 and Erk2 (IC50 = 3.7 µM & >10 µM, respectively). Does not affect the activity of several other protein kinases studied. Acutely sensitizes glycogen synthase activity in isolated skeletal muscle from insulin-sensitive lean Zucker and insulin-resistant Zucker diabetic fatty (ZDF) rats and can also augment insulin-stimulated glucose uptake in ZDF rats. However, it does not affect the basal glucose uptake rate. Induces a significant reduction in fasting hyperglycemia in diabetic and insulin-resistant db/db mice (~30 mg/kg, s.c.). Reduces Tau phosphorylation (Ser396) in the cortex and hippocampus of postnatal rats. Also shown to activate Wnt/β-catenin signaling and direct the differentiation of human pluripotent stem cells into cardiomyocytes.

Other Notes

Grigoryan, T., et al. 2013. Proc. Natl. Acad. Sci. USA110, 18174.
Lian, X., et al. 2012. Proc. Natl. Acad. Sci. USA109, E1848.
Selenica, M.L., et al. 2007. Br. J. Pharmacol.152, 959.
Ring, D.B., et al. 2003. Diabetes.52, 588.
Nikoulina, S.E., et al. 2002. Diabetes.51, 2190.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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