SB 431542 化学特性,用途語,生産方法
外観
白色～黄褐色、結晶性粉末～粉末
溶解性
メタノールに溶ける。
特長
細胞培養用途に安心して使用できるように、エンドトキシン試験、マイコプラズマ試験、細胞毒性確認済み。
特長
エンドトキシン試験、生菌数試験、マイコプラズマ試験済み原薬等登録原簿（マスターファイル）に登録済み。登録番号：228MF40016製造工程や分析法のバリデーション、変更管理を実施し、恒常的に安定した品質の製品を得られる体制で製造しています。
使用上の注意
滅菌品ではないため、溶解後フィルター滅菌してからご使用ください。
説明
SB-431542 is a potent and selective inhibitor of the TGF-
β1 receptor ALK5 (IC
50 = 94 nM). It is a less potent antagonist of ALK4 (IC
50 = 140 nM) and ALK7. It does not affect the BMP receptors ALK2, ALK3, ALK6, or a panel of other kinases tested. SB-431542 specifically blocks Smad signaling, reducing gene expression relevant to fibrosis and cancer. Through its effects on ALK/Smad signaling, SB-431542 suppresses renewal in embryonic and induced pluripotent stem cells and promotes their differentiation.
定義
ChEBI: A member of the class of benzamides that is 4-(imidazol-2-yl)benzamide carrying additional 1,3-benzodioxol-5-yl and pyridin-2-yl substituents at positions 4 and 5 respectively on the imidazole ring.
一般的な説明
A cell-permeable triarylimidazole compound that is shown to effectively inhibit cellular Smad2 phosphorylation (>90% inhibition by 10 μM inhibitor) upon vector-mediated expression of constitutively active ALK4, ALK5, or ALK7 in NIH 3T3 cells, while exhibiting little effect against Smad1 phosphorylation by other members of type I receptors for TGF-β in NIH 3T3 cultures expressing active ALK1, 2, 3, or 6. When tested directly in cell-free kinase assays, SB431542 is demonstrated to potently inhibit the activity of ALK4 and ALK5 (IC
50 = 140 nM and 94 nM, respectively) with no or much reduced potency toward a panel of 24 other kinases (IC
50 ≥10 μM in the presence of 10 μM ATP), including ALK2 and ALK6. Reported to improve the efficiency of 4-TF-induced human iPSCs generation from fibroblast cultures by >200-fold when used together with PD0325901 (Cat. No. 444966) and Thiazovivin (Cat. No. 420220).
生物活性
Potent and selective inhibitor of the transforming growth factor- β (TGF- β ) type I receptor activin receptor-like kinase ALK5 (IC 50 = 94 nM), and its relatives ALK4 and ALK7. Suppresses TGF- β -induced proliferation of human osteosarcoma cells. Stimulates proliferation, differentiation and sheet formation of ESC-derived endothelial cells.
SB 431542 上流と下流の製品情報
原材料
準備製品