Smad3 Inhibitor, SIS3

• CAT Number: I003897
• CAS Number: 521984-48-5
• Molecular Formula: C₂₈H₂₇N₃O₃ ∙ HCl
• Molecular Weight: 489.99
• Purity: ≥95%
• Synonyms: (E)-1-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one hydrochloride
• Target: SMAD
• Solubility: DMSO ≥ 30 mg/mL
• Storage: Store at -20C
• InChI: InChI=1S/C28H27N3O3.ClH/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;1H/b12-11+
• InChIKey: CDKIEBFIMCSCBB-CALJPSDSSA-N
• SMILES: CN1C(=C(C2=C1N=CC=C2)C=CC(=O)N3CCC4=CC(=C(C=C4C3)OC)OC)C5=CC=CC=C5.Cl

SIS3 is a potent and selective inhibitor of Smad3. a potent regulator of the human Nox4 promoter.target: Smad3SIS3 Reduces the TGF-β1-Dependent Increase in Phosphorylation and DNA Binding of Smad3. SIS3 has no effect on Smad2, p38 MAPK, ERK or PI 3-kinase signaling. SIS3 can block excessive ECM production from the TGF-β1-treated normal fibroblasts and scleroderma fibroblasts, the model of cells with autocrine TGF-β signaling in vitro.

Reference

[1]. Boudreau HE et al. Wild-type and mutant p53 differentially regulate NADPH oxidase 4 in TGF-β-mediated migration of human lung and breast epithelial cells. Br J Cancer. 2014 May 13;110(10):2569-82.
[2]. Jinnin M et al. Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-beta1-induced extracellular matrix expression. Mol Pharmacol. 2006 Feb;69(2):597-607.
[3]. Di Bernardini E et al. Endothelial lineage differentiation from induced pluripotent stem cells is regulated by microRNA-21 and transforming growth factor β2 (TGF-β2) pathways. J Biol Chem. 2014 Feb 7;289(6):3383-93.