WP1066

WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells when given at a concentration of 10 µM. It also induces apoptosis in U87-MG (IC50 = 5.6 µM) and U373-MG (IC50 = 3.7 µM) cells. WP1066 is orally bioavailable, crosses the blood-brain barrier, and demonstrates in vivo activity, including immune activation as indicated by the up-regulation of CD80 and CD86 and the induction of proliferation of effector T cells. In addition to inducing apoptosis in cancer cells, WP1066 suppresses vascular smooth muscle cell proliferation after vascular injury in mice and prevents seizures following brain injury in rats.Formal Name: 3-(6-bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2E-propenamide. CAS Number: 857064-38-1. Synonyms: STAT Inhibitor III. Molecular Formula: C17H14BrN3O. Formula Weight: 356.2. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7) (1:10): 0.09 mg/ml, DMSO: 16 mg/ml, Ethanol: 10 mg/ml. lambdamax: 261, 313 nm. SMILES: BrC1=CC=CC(/C=C(C#N)/C(N[C@@H](C)C2=CC=CC=C2)=O)=N1. InChi Code: InChI=1S/C17H14BrN3O/c1-12(13-6-3-2-4-7-13)20-17(22)14(11-19)10-15-8-5-9-16(18)21-15/h2-10,12H,1H3,(H,20,22)/b14-10+/t12-/m0/s1. InChi Key: VFUAJMPDXIRPKO-LQELWAHVSA-N.