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SIS3

Chemical Structure : SIS3

CAS No.: 521984-48-5

SIS3 (SIS 3, SIS-3)

Catalog No.: PC-43323Not For Human Use, Lab Use Only.

SIS3 (Specific Inhibitor of Smad3) is a potent, selective inhibitor of Smad3 function and TGF-β signaling, attenuates the TGF-β1-induced phosphorylation of Smad3 (IC50=3 uM) and interaction of Smad3 with Smad4.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SIS3 (Specific Inhibitor of Smad3) is a potent, selective inhibitor of Smad3 function and TGF-β signaling, attenuates the TGF-β1-induced phosphorylation of Smad3 (IC50=3 uM) and interaction of Smad3 with Smad4.
SIS3 decreases the levels of the DNA-Smad3 binding by approximately 50% at 3 uM; shows no effect on phosphorylated levels of Smad2, Smad4 and Smad7, as well as the phosphorylation of other signaling pathways, such as MAPK/p38.
SIS3 attenuates the effects of TGF-beta1 by reducing the transcriptional activity, also inhibits the myofibroblast differentiation of fibroblasts by TGF-beta1, completely diminishes the constitutive phosphorylation of Smad3 as well as the up-regulated type I collagen expression in scleroderma fibroblasts.

Physicochemical Properties

M.Wt 489.9932
Formula C28H28ClN3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

2-Propen-1-one, 1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-, hydrochloride (1:1), (2E)-

References

1. Jinnin M, et al. Mol Pharmacol. 2006 Feb;69(2):597-607.

2. Qureshi HY, et al. Biochim Biophys Acta. 2008 Sep;1783(9):1605-12.

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