TGF-β is a cell growth and differentiation factor that has roles in cancer, fibrosis, and numerous other pathologies.{20609,17350} TGF-β signals through two receptor tyrosine kinases, TGF-βRI and TGF-βRII. SD 208 is a potent inhibitor of TGF-βRI kinase (EC50 = 48 nM) that has minimal or no effect at a variety of other tyrosine or serine/threonine kinases, including TGF-βRII kinase.{27141} It blocks both autocrine and paracrine TGF-β signaling in glioma cells, inhibiting TGF-β-induced migration and invasion without affecting viability or proliferation.{27141} SD 208 is orally bioavailable and prevents TGF-β-induced Smad phosphorylation in spleens and brains of mice.{27141} It improves survival in mice with xenografted glioma by heightening the immune response against tumor cells and reverses bronchial hyperresponsiveness to allergens in ovalbumin-exposed mice.{27141,27142} SD 208 also suppresses TGF-β-induced differentiation of proliferating myofibroblasts and induces dedifferentiation in the absence of TGF-β.{27144,27143}
产品描述
A potent inhibitor of TGF-βRI kinase (EC50 = 48 nM) that has minimal or no effect at a variety of other kinases; blocks both autocrine and paracrine TGF-β signaling in glioma cells; is orally bioavailable and prevents TGF-β-induced Smad phosphorylation in spleens and brains of mice
