| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| S408658-1ml |
1ml |
现货  |
|
| 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。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 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 |
| 产品介绍 |
SB431542是一种有效的，选择性的ALK5抑制剂，IC50为94 nM，对ALK5的作用比对p38、 MAPK和其他激酶强100倍。A specific and selective inhibitor of TGF-β type I ALK receptors and Smad3. SB-431542被用于研究结直肠肿瘤细胞中血小板衍生生长因子受体B表达与TGF-β途径激活的相关性。它被用于研究TGF-β信号传导在调节细胞外基质 和成肌细胞分化中的作用。 Information 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. 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 lines：U87 and U251 cell lines Concentrations：0.3 μM Incubation Time：30 minutes Powder Purity:≥99% |
| 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 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 1 mg/mL (4.21 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|---|
| 熔点 | 214 °C(dec.) |
| 1. Jinyue Zhu, Weiqing Wang, Xia Wu. (2020) Isorhynchophylline exerts anti-asthma effects in mice by inhibiting the proliferation of airway smooth muscle cells: The involvement of miR-200a-mediated FOXC1/NF-κB pathway. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 521 (1055). [PMID:31733831] [10.1016/j.bbrc.2019.10.178] |
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