Smad3 Inhibitor, SIS3 - CAS 1009104-85-1
Catalog number: B0084-310534
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C28H27N3O3
Molecular Weight:
453.542
COA:
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Targets:
TGF-beta/Smad
Description:
Smad3 Inhibitor, SIS 3 is an inhibitor of SMAD3, which is a receptor-regulated intracellular protein that functions downstream of TGF-β as well as activin receptors and mediates their signaling. It plays an important role in cell proliferation, apoptosis, differentiation and formation of extracellular matrix. It is a cell-permeable pyrrolopyridine compound that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular 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.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-310534 25 mg $299 In stock
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Appearance:
Solid Powder
Synonyms:
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
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Shelf Life:
2 month in rt, long time
Boiling Point:
721.8±60.0 °C | Condition: Press: 760 Torr
Density:
1.21±0.1 g/cm3
InChIKey:
IJYPHMXWKKKHGT-UHFFFAOYSA-N
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
Canonical SMILES:
CN1C(=C(C2=C1N=CC=C2)C=CC(=O)N3CCC4=CC(=C(C=C4C3)OC)OC)C5=CC=CC=C5
1.[Reversal of stemness in multidrug-resistant hepatocellular carcinoma cells by SIS3].
Yan W1, Wen T1, Lin S1, Liu Z1, Yang W1, Wu G2. Zhonghua Zhong Liu Za Zhi. 2015 Oct;37(10):731-5.
OBJECTIVE: To investigate whether SIS3, a specific inhibitor of Smad3 phosphorylation, can reverse the stemness of multidrug-resistant(MDR) hepatocellular carcinoma cells.
2.Inhibition of development of laser-induced choroidal neovascularization with suppression of infiltration of macrophages in Smad3-null mice.
Iwanishi H1, Fujita N1, Tomoyose K1, Okada Y1, Yamanaka O1, Flanders KC2, Saika S1. Lab Invest. 2016 Mar 7. doi: 10.1038/labinvest.2016.30. [Epub ahead of print]
We evaluated the effects of the loss of Smad3 on the development of experimental argon laser-induced choroidal neovascularization (CNV) in mice. An in vitro angiogenesis model was also used to examine the role of transforming growth factor-β1 (TGFβ1)/Smad3 signaling in vessel-like tube formation by human umbilical vein endothelial cells (HUVECs). CNV was induced in eyes of 8-12-week-old B6.129-background Smad3-deficient (KO) mice (n=47) and wild-type (WT) mice (n=47) by argon laser irradiation. Results showed that the size of the CNV induced was significantly smaller in KO mice as compared with WT mice at day 14 as revealed by high-resolution angiography with fluorescein isothiocyanate-dextran. Immunohistochemistry and real-time reverse transcription-polymerase chain reaction of RNA extracted from laser-irradiated choroidal tissues were conducted on specimens at specific timepoints. Invasion of macrophages (F4/80+), but not neutrophils (myeloperoxidase+), and appearance of myofibroblasts (α-smooth muscle actin+) were suppressed in laser-irradiated KO tissues.
3.Glutamine protects cardiomyocytes from hypoxia/reoxygenation injury under high glucose conditions through inhibition of the transforming growth factor-β1-Smad3 pathway.
Zhang H1, Cui YC1, Li K1, Yang BQ1, Liu XP1, Zhang D1, Li H1, Wu AL1, Tang Y2. Arch Biochem Biophys. 2016 Apr 15;596:43-50. doi: 10.1016/j.abb.2016.03.003. Epub 2016 Mar 3.
Activation of transforming growth factor-β1 (TGF-β1)-Smad3 pathway aggravates myocardial ischemia/reperfusion injury (IRI). We previously showed that glutamine (Gln) protects cardiomyocytes from hypoxia/reoxygenation (H/R) injury under high glucose (HG) conditions. The aim of this study was to investigate whether Gln exerts its protective effect in H/R via inhibiting TGF-β1-Smad3 pathway. In vitro, H9c2 rat cardiomyocytes were treated with Gln with HG (33 mM) and/or H/R. We also performed in vivo experiments in which we treated normal and diabetic rats with Gln or solvent control following IRI. We assessed protein levels of TGF-β1, total Smad3, phosphorylated (p)-Smad3 and cleaved caspase-3 in H9c2 cells and rat myocardium by Western blotting. H9c2 cells treated with HG + H/R exhibited high apoptosis rates, as well as a highly activated TGF-β1-Smad3 pathway. TGF-β1 receptor inhibitor (SB431542) or Smad3 inhibitor (SIS3) reduced HG + H/R induced apoptosis.
4.Yap1 promotes the survival and self-renewal of breast tumor initiating cells via inhibiting Smad3 signaling.
Sun JG1,2, Chen XW2, Zhang LP2, Wang J2, Diehn M1. Oncotarget. 2016 Mar 1;7(9):9692-706. doi: 10.18632/oncotarget.6655.
Tumor initiating cells (TICs) serve as the root of tumor growth. After identifying TICs in spontaneous breast tumors of the MMTV-Wnt1 mouse model, we confirmed the specific expression and activation of Yes-associated protein 1 (Yap1) within TICs. To investigate the role of Yap1 in the self-renewal of breast TICs and the underlying mechanism, we sorted CD49fhighEpCAMlow cells as breast TICs. Active Yap1 with ectopic expression in breast TICs promoted their colony formation in vitro (p< 0.01) and self-renewal in vivo (p< 0.01), and led to a 4-fold increase in TIC frequency (p< 0.05).A conditional knock-out mouse was reconstructed to generate Yap1 knock-out breast tumors. The loss of Yap1 led to a dramatic growth disadvantage of breast TICs in vitro (p< 0.01) and in vivo (p< 0.01), and it also led to an over 200-fold decrease in TIC frequency (p< 0.01). The expression of active Yap1 was negatively correlated with that of phosphorylated Smad3 (p-Smad3).
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CAS 1009104-85-1 Smad3 Inhibitor, SIS3

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