Molecular structure of Smad3 Inhibitor, SIS3, CAS Number: 1009104-85-1
Smad3 Inhibitor, SIS3 (CAS 1009104-85-1)
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Alternate Names:
6,7-Dimethoxy-2-((2E)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-prop-2-enoyl))-1,2,3,4-tetrahydroisoquinoline
Application:
Smad3 Inhibitor, SIS3 is a cell permeable pyrrolopyridine and selective inhibitor of TGF-β1-dependent Smad3 phosphorylation
CAS Number:
1009104-85-1
Purity:
≥90%
Molecular Weight:
453.53
Molecular Formula:
C28H27N3O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
SMAD3, an intracellular protein regulated by receptors, plays a vital role in transmitting signals from TGF-β and activin receptors. It contributes to various cellular processes such as cell proliferation, differentiation, apoptosis, and the formation of the extracellular matrix. The effectiveness of Smad3 Inhibitor, SIS3, lies in its selective inhibition of TGF-β and activin signaling by suppressing the phosphorylation of Smad3 (IC50 = 3 µM). Notably, it does not impact the MAPK/p38, ERK, or PI3-kinase signaling pathways. Studies have demonstrated that Smad3 Inhibitor, SIS3 effectively reduces the expression of type 1 procollagen induced by TGF-β1 and inhibits myofibroblast differentiation in both normal dermal fibroblasts and scleroderma fibroblasts.
Smad3 Inhibitor, SIS3 (CAS 1009104-85-1) References
- SMAD3 is essential for transforming growth factor-β1-induced urokinase type plasminogen activator expression and migration in transformed keratinocytes. | Kocic, J., et al. 2012. Eur J Cancer. 48: 1550-7. PMID: 21798735
- Transforming growth factor-β stimulates β amyloid uptake by microglia through Smad3-dependent mechanisms. | Tichauer, JE. and von Bernhardi, R. 2012. J Neurosci Res. 90: 1970-80. PMID: 22715062
- Transforming growth factor-β1 mediates psoriasis-like lesions via a Smad3-dependent mechanism in mice. | Zhang, Y., et al. 2014. Clin Exp Pharmacol Physiol. 41: 921-32. PMID: 25132073
- Inhibition of development of laser-induced choroidal neovascularization with suppression of infiltration of macrophages in Smad3-null mice. | Iwanishi, H., et al. 2016. Lab Invest. 96: 641-51. PMID: 26950486
- Smad3 promotes cancer progression by inhibiting E4BP4-mediated NK cell development. | Tang, PM., et al. 2017. Nat Commun. 8: 14677. PMID: 28262747
- The preventive and therapeutic implication for renal fibrosis by targetting TGF-β/Smad3 signaling. | Zhang, Y., et al. 2018. Clin Sci (Lond). 132: 1403-1415. PMID: 29875262
- Combined Blockade of Smad3 and JNK Pathways Ameliorates Progressive Fibrosis in Folic Acid Nephropathy. | Jiang, M., et al. 2019. Front Pharmacol. 10: 880. PMID: 31447676
- Smad3 signalling affects high glucose-induced podocyte injury via regulation of the cytoskeletal protein transgelin. | Jiang, L., et al. 2020. Nephrology (Carlton). 25: 659-666. PMID: 32034833
- Puromycin aminonucleoside-induced podocyte injury is ameliorated by the Smad3 inhibitor SIS3. | Jiang, L., et al. 2020. FEBS Open Bio. 10: 1601-1611. PMID: 32583562
- Treatment of Hypertensive Heart Disease by Targeting Smad3 Signaling in Mice. | Meng, J., et al. 2020. Mol Ther Methods Clin Dev. 18: 791-802. PMID: 32953930
- Mitomycin C induces pulmonary vascular endothelial-to-mesenchymal transition and pulmonary veno-occlusive disease via Smad3-dependent pathway in rats. | Zhang, C., et al. 2021. Br J Pharmacol. 178: 217-235. PMID: 33140842
- A potential requirement for Smad3 phosphorylation in Notch-mediated EMT in colon cancer. | Clark, AG., et al. 2023. Adv Biol Regul. 88: 100957. PMID: 36739740
- SARS-CoV-2 N protein induces acute kidney injury in diabetic mice via the Smad3-Ripk3/MLKL necroptosis pathway. | Liang, L., et al. 2023. Signal Transduct Target Ther. 8: 147. PMID: 37029116
Inhibitor of:
BMP-5, COL12A1, COL4A2, Gm765, LTBP, Smad3, Smad5, and TIAF-1.Activator of:
ACTR-IB, EG625424, EG625464, Myocardin, Smad1, TGIF, and WFIKKN.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Smad3 Inhibitor, SIS3, 1 mg | sc-222318 | 1 mg | $252.00 |