AZD 2858

Glycogen synthase kinase 3beta (GSK3beta) was originally identified for its ability to constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis. It can also phosphorylate proteins that are relevant to osteogenesis and Alzheimer's disease, the latter for which it has earned the moniker, tau phosphorylating kinase. AZD 2858 is a pyrazine analog that inhibits GSK3beta with a Ki value of 4.9 nM. It crosses the blood brain barrier and inhibits tau phosphorylation in vitro with an IC50 value of 76 nM. AZD 2858 has also been shown to increase bone mass (via Wnt activation) in rats after a two-week treatment with a maximum effective oral dose of 20 mg/kg once daily. Furthermore, by inhibiting GSK3beta, AZD 2858 can stabilize beta-catenin in rat mesenchymal stem cells (EC50 = 234 nM), spurring osteoblast differentiation.Formal Name: 3-amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-2-pyrazinecarboxamide. CAS Number: 486424-20-8. Molecular Formula: C21H23N7O3S. Formula Weight: 453.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.1 mg/ml, DMSO: 5 mg/ml. lambdamax: 224, 304, 383 nm. SMILES: NC1=NC=C(C2=CC=C(S(N3CCN(C)CC3)(=O)=O)C=C2)N=C1C(NC4=CC=CN=C4)=O. InChi Code: InChI=1S/C21H23N7O3S/c1-27-9-11-28(12-10-27)32(30,31)17-6-4-15(5-7-17)18-14-24-20(22)19(26-18)21(29)25-16-3-2-8-23-13-16/h2-8,13-14H,9-12H2,1H3,(H2,22,24)(H,25,29). InChi Key: FHCSBLWRGCOVPT-UHFFFAOYSA-N.