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SIS3
- Smad3 inhibitor SIS3
- Soluble in DMSO
- MF: C28H27N3O3
- MW: 453.53
Description
SIS3 is a potent and selective inhibitor of Smad3 and TGF-β signaling. Inhibition by SIS3 leads to abrogation of the TGF-β1-induced production of extracellular matrix proteins in normal fibroblasts and scleroderma fibroblasts. Moreover, Smad3 inhibition attenuates resistance to anti-HER2 drugs in HER2-positive breast cancer cells.
More Information
| Parent CAS No. | 521985-36-4 |
|---|---|
| Chemical Name | (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 |
| SMILES | C1C=C2C(/C=C/C(=O)N3CC4C=C(OC)C(OC)=CC=4CC3)=C(C3C=CC=CC=3)N(C)C2=NC=1 |
| MFCD | N.A. |
| InChi | 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+ |
| InChiKey | IJYPHMXWKKKHGT-VAWYXSNFSA-N |
| CID | 10138988 |
| Short Description | Smad3 inhibitor |
References
- M Jinnin 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.
- Y Chihara et al. A small-molecule inhibitor of SMAD3 attenuates resistance to anti-HER2 drugs in HER2-positive breast cancer cells. Breast Cancer Res Treat. 2017 Nov;166(1):55-68.
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