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Alternative_name
(2E)-1-(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-propenone hydrochloride
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Description
A potent and selective inhibitor of Smad3 function. SIS3 selectively inhibits TGF-β1/ALK5-induced Smad3 phosphorylation. Also inhibits the TGF-β1 effect on type I procollagen expression at the transcriptional levels via the Smad3-binding site.
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CAS Number
521984-48-5
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Structure Available
Yes
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Salt Form
No
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Molecular Formula
C₂₈H₂₇N₃O₃ ∙ HCl
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Molecular Weight
489.99
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Cell Permeable
Yes
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Purity
≥98% by HPLC
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Solubilities
DMSO (>20 mg/ml)
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Handling
Protect from light and moisture
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Tag Line
A Smad3 inhibitor
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Storage Condition
-20°C
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Shipping Condition
gel pack
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Shelf Life
24 months
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MDL Number
MFCD09265258
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PubChem CID
16079005
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SMILES
CN1C(=C(C2=C1N=CC=C2)C=CC(=O)N3CCC4=CC(=C(C=C4C3)OC)OC)C5=CC=CC=C5.Cl
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InChi
InChI=1S/C28H27N3O3.ClH/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;1H/b12-11+;
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InChi Key
CDKIEBFIMCSCBB-CALJPSDSSA-N
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MSDS Available
Yes
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Additional description
Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
