SMAD3 Inhibitor, SIS3

SMAD3 is a receptor-regulated intracellular protein that functions downstream of TGF-beta and activin receptors and mediates their signaling, playing a role in cell proliferation, differentiation, apoptosis and formation of extracellular matrix. SMAD3 Inhibitor, SIS3 selectively inhibits TGF-beta and activin signaling by suppressing Smad3 phosphorylation (IC50 = 3 µM) without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways. It has been shown to reduce TGF-beta1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.Formal Name: 1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-2-propen-1-one. CAS Number: 1009104-85-1. Molecular Formula: C28H27N3O3. Formula Weight: 453.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:3): 0.2 mg/ml. lambdamax: 234, 292, 319 nm. SMILES: COC1=CC(CCN(C(/C=C/C2=C(C3=CC=CC=C3)N(C)C4=C2C=CC=N4)=O)C5)=C5C=C1OC. InChi Code: InChI=1S/C28H27N3O3/c1-30-27(19-8-5-4-6-9-19)22(23-10-7-14-29-28(23)30)11-12-26(32)31-15-13-20-16-24(33-2)25(34-3)17-21(20)18-31/h4-12,14,16-17H,13,15,18H2,1-3H3/b12-11+. InChi Key: IJYPHMXWKKKHGT-VAWYXSNFSA-N.