SB-431542
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Cat.No：IS1230 Solarbio
CAS：301836-41-9
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > TGF-β/Smad > SB-431542
Product Information
| CAS | 301836-41-9 |
| Name | SB-431542 |
| Molecular Formula | C22H16N4O3 |
| Molecular Weight | 384.39 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD05865244 |
| SMILES | O=C(C1=CC=C(C=C1)C2=NC(C3=CC=C4OCOC4=C3)=C(N2)C5=NC=CC=C5)N |
| Target Point | TGF-β Receptor;ALK |
| Passage | TGF-beta/Smad |
| Background | SB-431542 is a potent and selective ALK5 inhibitor; also a transforming growth factor beta receptor (TGF-beta Receptor) inhibitor. |
| Biological Activity | SB-431542 是一种有效，选择性的 ALK5 抑制剂，IC50 值为 94 nM；同时也是转化生长因子 β 受体 (TGF-β Receptor) 抑制剂。[1-6] |
| IC50 | 94nM(ALK5)[2] |
| In Vitro | SB-431542(1μM)显著降低TGF-β诱导的A498细胞中Smad蛋白的核积累。 SB-431542抑制TGF-β1诱导的胶原Iα1和PAI-1 mRNA，IC50值分别为60和50 nM。此外，SB-431542抑制TGF-β1诱导的纤连蛋白mRNA和蛋白，IC50值分别为62和22 nM [1]。 SB-431542(10μM)是内源性激活素和TGF-β信号传导的选择性抑制剂，但对NIH 3T3细胞中的BMP信号传导没有影响[2]。 TRKI，SB-431542，抑制TGF-β诱导的转录，基因表达，细胞凋亡和生长抑制。 SB-431542减弱TGF-β的肿瘤促进作用，包括TGF-β诱导的EMT，细胞运动，迁移和侵袭以及人癌细胞系中血管内皮生长因子的分泌。 SB-431542诱导不受TGF-β生长抑制的细胞不依赖锚定的生长，而它可以减少由TGF-β促进生长的细胞的集落形成[3]。 SB-431542(0.3μM)抑制MG63细胞中TGF-β诱导的细胞增殖[4]。 |
| In Vivo | SB-431542(10 mg/kg，ip)可降低肺转移，但不会显著改变原发性肿瘤4T1异种移植物的生长[5]。 |
| Cell Experiment | 将A498细胞以5，000至10，000个细胞/孔接种在96孔板中。将细胞血清剥夺24小时，然后用SB-431542处理48小时以评估细胞毒性。根据制造商的说明，通过用XTT标记和电子偶联试剂孵育细胞4小时来测定细胞活力。具有活性线粒体的活细胞产生橙色产物甲，，其使用平板读数器在A 450nm和A 500nm之间检测，参比波长大于600nm。吸光度值与活细胞数相关。 |
| Animal Experiment | 将1万个4T1细胞皮下注射到6周龄Balb/c雌性小鼠的第二乳房脂肪垫中。每周测量肿瘤两次，并使用以下公式计算体积：体积=宽度2×长度×0.52。将小鼠随机分配到两个处理组：对照，n = 14(20％DMSO/80％玉米油); SB-431542处理，n = 15(在20％DMSO/80％玉米油中10mg/kg体重，在肿瘤细胞接种后一天开始每周腹膜内注射三次。当第10天时的体积切除原发性肿瘤注射4T1细胞后，每天监测所有小鼠，4周后实施安乐死，解剖转移至快速冷冻进行进一步分析。 |
| Kinase Experiment | 将来自A549和HT29的每个库的总共100，000个细胞接种到12孔板的每个孔中。将细胞在含有0.2％FBS的培养基中培养18小时，然后在SB-431542(10μM)存在下在0.5mL培养基中用5ng/mL TGF-β1处理24小时。根据制造商的说明，将100μL每种上清液用于VEGF测定。对于TGF-β1ELISA，将来自A549，VMRC-LCD和HT29的每个库的100，000个细胞接种到12孔板的每个孔中并血清饥饿20小时。然后将细胞用SB-431542在0.5mL无血清RPMI培养基中处理24小时。根据制造商的说明，将100μL每种上清液培养基激活并用于TGF-β1测定。 |
| Data Literature Source | [1]. N. J. Laping，et al. Inhibition of Transforming Growth Factor (TGF)-β1-Induced Extracellular Matrix with a Novel Inhibitor of the TGF-β Type I Receptor Kinase Activity: SB-431542. [2]. Inman GJ，et al. 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. Mol Pharmacol，2002，62(1)，65-74. [3]. Halder SK，et al. A specific inhibitor of TGF-beta receptor kinase，SB-431542，as a potent antitumor agent for human cancers. Neoplasia，2005，7(5)，509-521. [4]. Matsuyama S，et al. SB-431542 and Gleevec inhibit transforming growth factor-beta-induced proliferation of human osteosarcoma cells. Cancer Res，2003，63(22)，7791-7798. [5]. Sato M，et al. Differential Proteome Analysis Identifies TGF-β-Related Pro-Metastatic Proteins in a 4T1 Murine Breast Cancer Model. PLoS One. 2015 May 18;10(5):e0126483. [6]. 'Ma J，et al. Growth differentiation factor 11 improves neurobehavioral recovery and stimulates angiogenesis in rats subjected to cerebral ischemia/reperfusion. Brain Res Bull. 2018 Feb 9;139:38-47.' |
| Unit | Piece |
| Specification | 5mg 10mg 50mg |
SB-431542是一种有效，选择性的 ALK5 抑制剂，同时也是TGF-β Receptor抑制剂。是脑和血管类器官分化培养基的组成成分。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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