SB431542 is a potent and selective inhibitor ofALK5withIC50of 94 nM in a cell-free assay, 100-fold more selective for ALK5 than p38 MAPK and other kinases.
In vitro

SB 431542 inhibits the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are responsible for the phosphorylation of Smad2. SB 431542 has little effect on ALK1, ALK2, ALK3, and ALK6, which show phosphorylation of Smad1. SB 431542 is a selective inhibitor of endogenous activin but has no apparent effect on BMP signaling. SB 431542 could induce both Smad2/Smad4- and Smad3/Smad4-dependent transcription. In A498 cells, SB 431542 inhibits both TGF-β1-induced collagen Iα1 and PAI-1 mRNA with IC50 of 60 nM and 50 nM, respectively. In addition, SB 431542 inhibits production of TGF-β1-induced fibronectin mRNA and protein with IC50 of 62 nM and 22 nM, respectively. SB 431542 blocks the TGF-β-mediated growth factors, including PDGF-A, FGF-2 and HB-EGF, leading to an increase in proliferation of MG63 cells. SB 431542 also inhibits TGF-β-induced c-Myc and p21 ^WAF1/CIP1. SB 431542 significantly suppresses TGF-β-induced G1 arrest, leading to accumulation of cells in the S phase of the cell cycle in FET, RIE, and Mv1Lu cells. SB 431542 also inhibits TGF-β-induced epithelial to mesenchymal transition (EMT) in NMuMG and PANC-1 cells. SB 431542 significantly elevates the expression of CD86 in BM-DCs and that of CD83 within CD11c+ cells suppressed by TGF-β. SB 431542 is able to induce NK activity through functional maturation and IL-12 production of human DCs.

In vivo

SB 431542 triggers cytotoxic T lymphocyte (CTL) activities in the colon-26 carcinoma models and is most likely to produce antitumor immunological outcomes through alteration of DC function suppressed by TGF-β.
Cell Data

cell lines：U87 and U251 cell lines

Concentrations：0.3 μM

Incubation Time：30 minutes

Powder Purity:≥99%

规格

英文别名

4-(4-(benzo[d][1,3]dioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl)benzamide

规格或纯度

Moligand™, 10mM in DMSO

英文名称

SB431542

生化机理

SB431542 是一种强效的 ALK5 选择性抑制剂，在无细胞实验中的 IC50 值为 94 nM，对 ALK5 的选择性是 p38 MAPK 和其他激酶的 100 倍。

储存条件

-80℃储存

运输条件

特低温运输

作用类型

抑制剂

作用机制

激活素 A 受体 1C 型抑制剂；转化生长因子 beta 受体 1 抑制剂

名称和识别符

EC号

188-365-3

分子类型

小分子

Isomeric SMILES

C1OC2=C(O1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5

分子量

384.39

技术文档

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高级数据

关联靶点（人）

TGFBR1 Tchem TGF-β受体1型(TGF-beta receptor type-1) (2 活性数据)

点击查看靶蛋白信息： TGFBR1

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

化学和物理性质

溶解性

Solubility (25°C) In vitro DMSO: 1 mg/mL (4.21 mM); Water: Insoluble; Ethanol: Insoluble;

熔点

214 °C(dec.)

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批号(Lot Number)	证书类型	货号
A2305010	分析证书	S408658

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