EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #72232_C
激活素/BMP/TGF-β 通路抑制剂；抑制 ALK4、ALK5 和 ALK7
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总览
SB431542 是一种选择性强效 TGF-β/Activin/NODAL 通路抑制剂，通过竞争 ATP 结合位点抑制 ALK5（IC₅₀ = 94 nM）、ALK4（IC₅₀ = 140 nM）和 ALK7。它不抑制 BMP I 型受体 ALK2、ALK3 和 ALK6（Inman et al.; Laping et al.）。本产品以水合物形式提供。
重编程
·取代 SOX2，将小鼠成纤维细胞重编程为诱导多能干细胞 (iPS) （Ichida et al.）。
·与 PD0325901 和 Thiazovivin 联合使用，可提高将人体细胞重编程为 iPS 细胞的效率（Lin et al.）。
·与 CHIR99021、ISX-9、Forskolin 和 I-BET151 联合使用，可将成纤维细胞直接谱系重编程为成熟神经元（Li et al.）。
分化
·与 LDN193189 或 Noggin 联合使用，可促进人 PSC 向神经祖细胞分化（Chambers et al. 2009, Chambers et al. 2012）。
·促进小鼠胚胎干 (ES) 来源内皮细胞的增殖和片状结构形成（Watabe et al.）。
·增强小鼠和人 PSC 向心肌细胞的分化（Kattman et al.）。
·抑制人多能干细胞 (PSC) 的自我更新并促进其分化，表明 TGF-β/Activin/NODAL 通路在其维持中的重要性（James et al., Vallier et al.）。
细胞类型
心肌细胞，PSC衍生，内皮细胞，神经细胞，PSC衍生，神经干/祖细胞，神经元
种属
人，小鼠，非人灵长类，其他物种，大鼠
应用
分化，重编程
研究领域
神经科学，干细胞生物学
CAS 编号
不适用
化学式
• C₂₂H₁₆N₄O₃
• XH₂O
纯度
≥98%
通路
Activin/Nodal/TGFβ
靶点
ALK
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
应用领域
本产品专为以下研究领域设计，适用于工作流程中的高亮阶段。探索这些工作流程，了解更多我们为各研究领域提供的其他配套产品。
相关材料与文献
技术资料 (5)
文献 (11)
Inhibition of transforming growth factor (TGF)-beta1-induced extracellular matrix with a novel inhibitor of the TGF-beta type I receptor kinase activity: SB-431542.
Molecular pharmacology 2002 JUL
Abstract
Transforming growth factor beta1 (TGF-beta1) is a potent fibrotic factor responsible for the synthesis of extracellular matrix. TGF-beta1 acts through the TGF-beta type I and type II receptors to activate intracellular mediators,such as Smad proteins,the p38 mitogen-activated protein kinase (MAPK),and the extracellular signal-regulated kinase pathway. We expressed the kinase domain of the TGF-beta type I receptor [activin receptor-like kinase (ALK)5] and the substrate,Smad3,and determined that SB-431542 is a selective inhibitor of Smad3 phosphorylation with an IC50 of 94 nM. It inhibited TGF-beta1-induced nuclear Smad3 localization. The p38 mitogen-activated protein kinase inhibitors SB-203580 and SB-202190 also inhibit phosphorylation of Smad3 by ALK5 with IC50 values of 6 and 3 microM,respectively. This suggests that these p38 MAPK inhibitors must be used at concentrations of less than 10 microM to selectively address p38 MAPK mechanisms. However,the p38 MAPK inhibitor SB-242235 did not inhibit ALK5. To evaluate the relative contribution of Smad signaling and p38 MAPK signaling in TGF-beta1-induced matrix production,the effect of SB-431542 was compared with that of SB-242235 in renal epithelial carcinoma A498 cells. All compounds inhibited TGF-beta1-induced fibronectin (FN) mRNA,indicating that FN synthesis is mediated in part via the p38 MAPK pathway. In contrast,SB-431542,but not the selective p38 MAPK inhibitor SB-242235,inhibited TGF-beta1-induced collagen Ialpha1 (col Ialpha1). These data indicate that some matrix markers that are stimulated by TGF-beta1 are mediated via the p38 MAPK pathway (i.e.,FN),whereas others seem to be activated via ALK5 signaling independent of the p38 MAPK pathway (i.e.,col Ialpha1).
SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7.
Molecular pharmacology 2002 JUL
Abstract
Small molecule inhibitors have proven extremely useful for investigating signal transduction pathways and have the potential for development into therapeutics for inhibiting signal transduction pathways whose activities contribute to human diseases. Transforming growth factor beta (TGF-beta) is a member of a large family of pleiotropic cytokines that are involved in many biological processes,including growth control,differentiation,migration,cell survival,adhesion,and specification of developmental fate,in both normal and diseased states. TGF-beta superfamily members signal through a receptor complex comprising a type II and type I receptor,both serine/threonine kinases. Here,we characterize a small molecule inhibitor (SB-431542) that was identified as an inhibitor of activin receptor-like kinase (ALK)5 (the TGF-beta type I receptor). We demonstrate that it inhibits ALK5 and also the activin type I receptor ALK4 and the nodal type I receptor ALK7,which are very highly related to ALK5 in their kinase domains. It has no effect on the other,more divergent ALK family members that recognize bone morphogenetic proteins (BMPs). Consistent with this,we demonstrate that SB-431542 is a selective inhibitor of endogenous activin and TGF-beta signaling but has no effect on BMP signaling. To demonstrate the specificity of SB-431542,we tested its effect on several other signal transduction pathways whose activities depend on the concerted activation of multiple kinases. SB-431542 has no effect on components of the ERK,JNK,or p38 MAP kinase pathways or on components of the signaling pathways activated in response to serum.
TGF-beta receptor kinase inhibitor enhances growth and integrity of embryonic stem cell-derived endothelial cells.
The Journal of cell biology 2003 DEC
Abstract
Recent findings have shown that embryonic vascular progenitor cells are capable of differentiating into mural and endothelial cells. However,the molecular mechanisms that regulate their differentiation,proliferation,and endothelial sheet formation remain to be elucidated. Here,we show that members of the transforming growth factor (TGF)-beta superfamily play important roles during differentiation of vascular progenitor cells derived from mouse embryonic stem cells (ESCs) and from 8.5-days postcoitum embryos. TGF-beta and activin inhibited proliferation and sheet formation of endothelial cells. Interestingly,SB-431542,a synthetic molecule that inhibits the kinases of receptors for TGF-beta and activin,facilitated proliferation and sheet formation of ESC-derived endothelial cells. Moreover,SB-431542 up-regulated the expression of claudin-5,an endothelial specific component of tight junctions. These results suggest that endogenous TGF-beta/activin signals play important roles in regulating vascular growth and permeability.
更多信息
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
|---|---|
| Cas Number | Not applicable |
| Chemical Formula | C₂₂H₁₆N₄O₃ • XH₂O |
| 纯度 | ≥ 98% |
| Target | ALK |
| Pathway | Activin/Nodal/TGFβ |
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