Биологическая активность
SMAD3 is a рецептор-regulated intracellular protein that functions downstream of TGF-β and activin receptors and mediates their signaling, playing a role in клетка proliferation, differentiation, apoptosis and formation of extracellular matrix. Smad3 ингибитор, SIS3 is a клетка-permeable pyrrolopyridine compound that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated клеточный signaling with no effect on Smad2, p38 MAPK, ERK, or PI 3-K signaling. 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.
Оригинал на английском
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 is a cell-permeable pyrrolopyridine compound that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling with no effect on Smad2, p38 MAPK, ERK, or PI 3-K signaling. 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.
Химические свойства
- CAS №
- 1009104-85-1
- Брутто-формула
- C₂₈H₂₇N₃O₃
- Мол. масса
- 453.53 г/моль
- SMILES
- CN1C2C(=CC=CN=2)C(/C=C/C(N2CCC3=C(C=C(C(OC)=C3)OC)C2)=O)=C1C1=CC=CC=C1
- Синонимы
- SMAD3 Inhibtor, SIS 3; 1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3-(1-methyl-2-phenylpyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one; SMAD3 Inhibitor, SIS3; SIS3 free base; Smad3 Inhibitor
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.