GSK-3 Inhibitor XVI A compound that acts as potent, ATP-competitive & highly selective GSK-3 inhibitor

GSK-3 Inhibitor XVI (CAS 252917-06-9)

GSK-3 Inhibitor XVI | CAS 252917-06-9 is rated 5.0 out of 5 by 1.
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Synonym: 6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile
Application: A compound that acts as potent, ATP-competitive & highly selective GSK-3 inhibitor
CAS Number: 252917-06-9
Purity: >98%
Molecular Weight: 465.34
Molecular Formula: C22H18Cl2N8
* Refer to Certificate of Analysis for lot specific data (including water content).
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GSK-3 Inhibitor XVI is a cell-permeable aminopyrimidine compound that acts as potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC50 = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively). CHIR99021 exhibits little to no activity toward 46 other enzymes (IC50 >8.8 μM against 20 kinases and Ki ≥5 μM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (Kd ~4 μM).

Physical State :
Solid
Solubility :
Soluble in DMSO (10 mg/ml), water (<1 mg/ml) at 25° C, and ethanol (<1 mg/ml) at 25° C.
Storage :
Store at 4° C
Melting Point :
316.33° C (Predicted)
Boiling Point :
784.08° C at 760 mmHg (Predicted)
Density :
1.48 g/cm3 (Predicted)
Refractive Index :
n20D 1.7 (Predicted)
IC50 :
GSK-3α: IC50 = 10 nM; GSK-3β: IC50 = 6.7 nM; kinases: IC50 = >8.8 µM; Glycogen synthase kinase-3 beta: EC5050 = 1.5 µM (human); G2/mitotic-specific cyclin B1: IC50 = 8.8 µM (human); activates glycogen synthesis: EC5050 = 0.8 µM (CHO-IR cells)
Ki Data :
non-kinase enzymes: Ki= ≥5 µM
pK Values :
pKa: 11.92 (Predicted), pKb: 4.05 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
9956119
MDL Number :
MFCD11846251
SMILES :
CC1=CN=C(N1)C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)Cl)NCCNC4=NC=C(C=C4)C#N

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Certificate of Analysis

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GSK-3 Inhibitor XVI  Product Citations

See how others have used GSK-3 Inhibitor XVI. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 25843659  Zimmermann, K. et al. 2015. Free Radic. Biol. Med. 88: 417-426.

PMID: # 24021571  Wu, Y. et al. 2013. Exp. Cell Res. 319: 2684-99.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Various publications have cited GSK Various publications have cited GSK-3 Inhibitor XVI as a potent, cell-permeable aminopyrimidine compound shown to selectively inhibit GSK-3, with little effect on similar enzymes. -SCBT Publication Review
Date published: 2015-02-18
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