| Identification | Back Directory | [Name]
Smad3 Inhibitor, SIS3 | [CAS]
1009104-85-1 | [Synonyms]
SIS3 free base
Smad3 Inhibitor
Smad3 Inhibitor, SIS3
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)- | [Molecular Formula]
C28H27N3O3 | [MDL Number]
MFCD24368989 | [MOL File]
1009104-85-1.mol | [Molecular Weight]
453.53 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 Smad2p38 mitogen-activated protein kinase (MAPK)extracellular-signal-regulated kinase (ERK)or phosphoinositide 3-kinase (PI3K) signaling. Through its inhibitory functionSIS3 regulates fibrosisapoptosisand inflammation in mouse unilateral ureteral obstruction (UUO) kidneys. ThereforeSIS3 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). |
| [storage]
Store at -20°C |
|
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|