SMAD3 Inhibitor, SIS3 是一种有效的选择性 Smad3 磷酸化抑制剂。
| Cas No. | 1009104-85-1 |
| 化学名 | 1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-2-propen-1-one |
| Canonical SMILES | COC1=CC(CCN(C(/C=C/C2=C(C3=CC=CC=C3)N(C)C4=C2C=CC=N4)=O)C5)=C5C=C1OC |
| 分子式 | C28H27N3O3 |
| 分子量 | 453.5 |
| 溶解度 | 30mg/mL in ethanol, or in DMSO, or in DMF |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | SMAD3 is a receptor-regulated intracellular protein that functions downstream of TGF-β and activin receptors and mediates their signaling, playing a role in cell proliferation, differentiation, apoptosis and formation of extracellular matrix. SMAD3 Inhibitor, SIS3 selectively inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation (IC50 = 3 µM) without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways.[1] 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.[1] Reference:
[1]. Jinnin, M., Ihn, H., and Tamaki, K. Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-β1-induced extracellular matrix expression. Molecular Pharmacology 69(2), 597-607 (2006). |
