SB 431542
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SB431542是一种选择性的和ATP竞争性的活化素受体样激酶5（ALK5）抑制剂，IC50值为94 nM[1]。
SB431542在一系列点击率筛选中具有最有力的功效。在A498细胞中，SB431542抑制TGF-β1诱导的mRNA形成，IC50值为50 nM。SB431542也显著减少TGF-β诱导的Smad蛋白的核积累，IC50值为40 nM。SB431542是一种选择性的ALK4、ALK5和ALK7抑制剂，抑制Smad2的磷酸化。而在10 μM浓度时对ALK1、ALK2和ALK6没有显著的抑制效果，对ALK3具有微弱的抑制效应[1，2]。
参考文献：
[1] Callahan J F, Burgess J L, Fornwald J A, et al. Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1) type 1 receptor (ALK5). Journal of medicinal chemistry, 2002, 45(5): 999-1001.
[2] Inman G J, Nicolás F J, Callahan J F, et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Molecular pharmacology, 2002, 62(1): 65-74.
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| Physical Appearance | A solid |
| Storage | Store at RT |
| M.Wt | 384.39 |
| Cas No. | 301836-41-9 |
| Formula | C22H16N4O3 |
| Solubility | insoluble in H2O; ≥10.06 mg/mL in EtOH with ultrasonic; ≥19.22 mg/mL in DMSO |
| Chemical Name | 4-[4-(1,3-benzodioxol-5-yl)-5-pyridin-2-yl-1H-imidazol-2-yl]benzamide |
| SDF | Download SDF |
| Canonical SMILES | C1OC2=C(O1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验: [1] | |
|
细胞系 |
D54MG、U87MG和U373MG细胞 |
|
制备方法 |
该化合物在DMSO中的溶解度大于10 mM，若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
|
反应条件 |
10 μM，24 hours |
|
实验结果 |
0.1和1 μmol/L的SB-431542 适度影响DNA合成，但是在10μmol/L时，D54MG、U87MG和U373MG细胞的胸苷掺入减少60％至70％。通过直接观察或碘化丙锭流式细胞术分析，没有检测到SB-431542处理的凋亡性细胞死亡的证据。因此，SB-431542被用于抑制所测试的恶性胶质瘤细胞系的增殖。 |
| 动物实验: [2] | |
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动物模型 |
注射colon-26细胞的BALB/c小鼠 |
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给药剂量 |
腹腔注射，1 μM |
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实验结果 |
与单独的载体相比，腹腔注射SB-431542引发针对colon-26靶标的CTL活性。此外，与单独的OK-432相比，SB和toll样受体4的配体OK-432共同使用，针对colon-26细胞的CTL活性更有效。因此，SB-431542可能通过改变由TGFβ抑制的DC功能，从而产生抗肿瘤免疫学结果。 |
|
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
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References: [1] Hjelmeland M D, Hjelmeland A B, Sathornsumetee S, et al. SB-431542, a small molecule transforming growth factor-β-receptor antagonist, inhibits human glioma cell line proliferation and motility. Molecular Cancer Therapeutics, 2004, 3(6): 737-745. [2] Tanaka H, Shinto O, Yashiro M, et al. Transforming growth factor b signaling inhibitor, SB-431542, induces maturation of dendritic cells and enhances anti-tumor activity. Oncology reports, 2010, 24: 1637-1643. |
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| 描述 | SB431542是一种有效的和选择性的ALK5抑制剂，IC50值为94 nM，对ALK5的选择性比对p38 MAPK和其它激酶高100倍。 | |||||
| 靶点 | ALK5 | |||||
| IC50 | 94 nM | |||||
质量控制和MSDS
- 批次:
化学结构
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