SIS3 hydrochloride | CAS 521984-48-5

Element: hydrochloride sis3

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C-S » Chemicals » sis-hydrochloride-PX45336

Identification

SIS3 hydrochloride

CAS:

521984-48-5

EINECS:

Molecular Formula:

C₂₈H₂₇N₃O₃.HCl

MDL:

MFCD09265258

SMILES:

CN1C(=C(C2=C1N=CC=C2)/C=C/C(=O)N3CCC4=CC(=C(C=C4C3)OC)OC)C5=CC=CC=C5.Cl

Synonym:

sis3 hcl ; sis3 hydrochloride ; (2e)-1-(6,7-dimethoxy-3,4-dihydro-1h-isoquinolin-2-yl)-3-(1-methyl-2-phenyl-1h-pyrrolo[2,3-b]pyridin-3-yl)-propenone hydrochloride ; sis3

Description

SIS3 hydrochloride is a specific inhibitor of Smad3 phosphorylation via inhibiting the effects of TGF-β1. Studies conducted on scleroderma fibroblasts indicate that SIS3 hydrochloride suppresses type I collagen up-regulation. In addition, SIS3 hydrochloride inhibits Smad-responsive p3TP promoter constructs activation. These studies suggest that SIS3 hydrochloride reduces DNA binding of Smad3 and that pretreatment with SIS3 hydrochloride decreases DNA binding by 50%. SIS3 hydrochloride also interferes with the interaction between contransfected Smad3 and Smad4. Furthermore, SIS3 hydrochloride reestablishes myofibroblast differentiation of scleroderma fibroblasts via reducing expression of α-SMA in these fibroblasts.