VTX-27

VTX-27 is a PKCtheta inhibitor (Ki = 0.08 nM). It is selective for PKCtheta over PKCalpha, -betaI, -betaII, -gamma, -delta, -epsilon, -eta, -µ, and -zeta with Ki values ranging from 1 to >5,000 nM as well as a panel of seven kinases from the Src, spleen tyrosine kinase (Syk), Tec, and MAP kinase families (Kis = >1,000 nM for all). VTX-27 inhibits CD28-induced IL-2 release in isolated human peripheral blood mononuclear cells (PBMCs, IC50 = 11 nM). Oral administration of VTX-27 (12.5, 25, and 50 mg/kg) prevents staphylococcal enterotoxin B-induced increases in IL-2 plasma levels in mice.Formal Name: (alphaR,2S)-4-[3-chloro-5-fluoro-6-(1H-pyrazolo[3,4-b]pyridin-3-yl)-2-pyridinyl]-alpha-methyl-alpha-(1-methylethyl)-2-piperazinemethanol. CAS Number: 1321924-70-2. Molecular Formula: C20H24ClFN6O. Formula Weight: 418.9. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. SMILES: FC1=C(N=C(N2C[C@@](NCC2)([H])[C@](C)(O)C(C)C)C(Cl)=C1)C3=NNC4=NC=CC=C34. InChi Code: InChI=1S/C20H24ClFN6O/c1-11(2)20(3,29)15-10-28(8-7-23-15)19-13(21)9-14(22)17(25-19)16-12-5-4-6-24-18(12)27-26-16/h4-6,9,11,15,23,29H,7-8,10H2,1-3H3,(H,24,26,27)/t15-,20+/m0/s1. InChi Key: HXWARSZQGAFXJM-MGPUTAFESA-N.