SMAD3|CAS 1009104-85-1|DC Chemicals

Cas No.:	1009104-85-1
Chemical Name:	SMAD3 Inhibtor, SIS 3
Synonyms:	SMAD3 Inhibtor, SIS 3;1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3-(1-methyl-2-phenylpyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one;SMAD3 Inhibitor, SIS3;SIS3 free base;Smad3 Inhibitor
SMILES:	CN1C2C(=CC=CN=2)C(/C=C/C(N2CCC3=C(C=C(C(OC)=C3)OC)C2)=O)=C1C1=CC=CC=C1
Formula:	C₂₈H₂₇N₃O₃
M.Wt:	453.532286882401
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	SMAD3 is a receptor-regulated intracellular protein that functions downstream of TGF-β and activin receptors and mediates their signaling, playing a role in cell proliferation, differentiation, apoptosis and formation of extracellular matrix. Smad3 Inhibitor, SIS3 is a cell-permeable pyrrolopyridine compound that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling with no effect on Smad2, p38 MAPK, ERK, or PI 3-K signaling. It has been shown to reduce TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.
Target:	Smad3, ALK-5[1]
In Vitro:	SIS3 free base (0.3-10 μM; for 1 hour) attenuates the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4[1]. Western Blot Analysis[1] Cell Line: Human dermal fibroblasts Concentration: 0.3, 1, 3, 10 μM Incubation Time: For 1 hour Result: Attenuated the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4.
References:	[1]. 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. Epub 2005 Nov 15.

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