Smad3 Inhibitor, SIS3 manufacturers
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| | Smad3 Inhibitor, SIS3 Basic information |
| Product Name: | Smad3 Inhibitor, SIS3 | | Synonyms: | Smad3 Inhibitor;Smad3 Inhibitor, SIS3;SIS3 free base;SMAD3 Inhibtor, SIS 3;(E)-1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-3-pyrrolo[2,3-b]pyridyl)-2-propen-1-one;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)-;SIS-3 free base,SIS3 free base;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 | | CAS: | 1009104-85-1 | | MF: | C28H27N3O3 | | MW: | 453.53 | | EINECS: | | | Product Categories: | Specific Inhibitor of Smad3, SIS3 | | Mol File: | 1009104-85-1.mol |  |
| | Smad3 Inhibitor, SIS3 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH 7.2) (1:3): 0.2 mg/ml | | form | A crystalline solid | | color | off-white | | 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 | | InChIKey | IJYPHMXWKKKHGT-UHFFFAOYSA-N | | SMILES | [n]1(c2ncccc2c(c1c5ccccc5)C=CC(=O)N3CCc4c(cc(c(c4)OC)OC)C3)C |
| WGK Germany | WGK 1 | | Storage Class | 11 - Combustible Solids |
| | Smad3 Inhibitor, SIS3 Usage And Synthesis |
| Uses | SMAD3 Inhibitor, SIS3 selectively inhibits TGF-β and activin. 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. | | Definition | ChEBI: An enamide resulting from the formal condensation of the amino group of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline with the carboxy group of (2E)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)acrylic
cid. | | Biological Activity | Primary Target
TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling', 'The specific inhibitor of Smad3 (SIS3) is a pyrrolopyridine compound. It selectively blocks transforming growth factor (TGF)-β1-dependent mothers against decapentaplegic homolog 3 (Smad3) phosphorylation and Smad3-mediated cellular pathway without affecting Smad2, p38 mitogen-activated protein kinase (MAPK), extracellular-signal-regulated kinase (ERK), or phosphoinositide 3-kinase (PI3K) signaling. Through its inhibitory function, SIS3 regulates fibrosis, apoptosis, and inflammation in mouse unilateral ureteral obstruction (UUO) kidneys. Therefore, SIS3 can be an effective drug in further anti-fibrosis treatment of kidney disease. | | in vivo | E/Z-SIS3 free base (2 mg/kg, i.p.) inhibits smad3 phosphorylation and levels of TGF-β1, ameliorates bleomycin (BLM)-induced pulmonary fibrosis (PF) and inflammation in C57BL/6J mice[1]. | Animal Model: | BLM-induced PF in C57BL/6J mice[1] | | Dosage: | 2 mg/kg | | Administration: | i.p., every two days for 3 weeks | | Result: | Inhibited the fibrosis and collagen deposition in lung.
Reduced numbers of lymphocytes, macrophages, and neutrophils in bronchoalveolar Lavage (BAL). |
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| | Smad3 Inhibitor, SIS3 Preparation Products And Raw materials |
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