CHIR-98014A selective and ATP-competitive inhibitor of GSK-3β

CHIR-98014 (CAS 252935-94-7)

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Synonym: N6-[2-[[4-(2,4-dichlorophenyl)-5-(1H-imidazol-1-yl)-2-pyrimidinyl]amino]ethyl]-3-nitro-2,6-Pyridinediamine
Application: A selective and ATP-competitive inhibitor of GSK-3β
CAS Number: 252935-94-7
Molecular Weight: 486.31
Molecular Formula: C20H17Cl2N9O2
* Refer to Certificate of Analysis for lot specific data (including water content).

CHIR-98014 is a selective and ATP-competitive inhibitor of Glycogen Synthase Kinase 3β(GSK-3β) with Ki values of 0.87 nM. In addition, CHIR-98014 displays 500 to greater than 1000-fold selectivity towards GSK3 than other protein kinases such as cdc2 and erk2. The inhibitory effects of CHIR-98014 are similar for both α and β isoforms of GSK-3.

Physical State :
Solid
Solubility :
Soluble in DMSO (4 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), ethanol (<1 mg/ml at 25 °C), and 15% Captisol/citrate vehicle (30 mg/ml at 25 °C).
Storage :
Store at -20° C
Boiling Point :
~795.1 °C at 760 mmHg (Predicted)
Density :
~1.6 g/cm3 (Predicted)
Refractive Index :
n20D 1.76 (Predicted)
IC50 :
GSK-3 β: IC50 = 0.58 nM; GSK-3 α: IC50 = 0.65 nM
Ki Data :
GSK-3 β: Ki= 0.87 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
53396311
MDL Number :
MFCD10565922
SMILES :
C1=CC(=C(C=C1Cl)Cl)C2=Nxs(=NC=C2N3C=CN=C3)NCCNC4=NC(=C(C=C4)[N+](=O)[O-])N

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Certificate of Analysis

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CHIR-98014  Product Citations

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Citations 1 to 1 of 1 total

PMID: # 30508787  Fleischer, S.|Jahnke, HG.|Fritsche, E.|Girard, M.|Robitzki, AA.| et al. 2019. Biosens Bioelectron. 126: 624-631.

Citations 1 to 1 of 1 total
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