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SB-431542

SB-431542

产品编号 T1726   CAS 301836-41-9
别名: 4-[4-(1,3-苯并二唑-5-基)-5-(2-吡啶基)-1H-咪唑-2-基]-苯酰胺水合物, SB 431542

SB-431542 是一种 ALK5/TGF-β type I Receptor 的抑制剂 (IC50=94 nM),具有选择性。SB 431542 对 ALK4 和 ALK7 也有抑制活性,但对其他蛋白没有抑制作用。SB 431542 可以用于干细胞的诱导分化。

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SB-431542 Chemical Structure
SB-431542, CAS 301836-41-9
规格 价格/CNY 折后价 货期 数量
5 mg ¥ 412 ¥ 206 现货
10 mg ¥ 667 ¥ 333 现货
50 mg ¥ 2,530 ¥ 1,265 现货
100 mg ¥ 3,570 ¥ 1,785 现货
1 mL * 10 mM (in DMSO) ¥ 519 ¥ 259 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: SB-431542 (T1726)
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纯度: 100%
纯度: 99.87%
纯度: 99.09%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 SB-431542 is an inhibitor of ALK5/TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.
靶点活性 ALK5:94 nM, ALK4:140 nM
体外活性 方法:人肾细胞 293T、人类结肠癌来源的非致瘤性细胞 FET 和人肺腺癌细胞 A549 用 SB-431542 (2-10 μM) 和 TGF-β1 (12.5 ng/mL) 处理 1 h,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:TGF-β1 诱导了 Smad2/3 和 Smad4 之间的复合物形成。SB-431542 以剂量依赖的方式,通过阻断 TGF-β 诱导的磷酸化和Smad2/3的激活,阻断复合物形成。[1]
方法:人胶质母细胞瘤细胞 D54MG 用 SB-431542 (1-10 μM) 处理 24 h,使用 Transwell 方法检测细胞迁移情况。
结果: SB-431542抑制 TGF-βRI 信号传导以浓度依赖的方式阻断 D54MG 细胞的细胞迁移。[2]
方法:人多能干细胞 hESCs 用含 SB-431542 (10 nM) 和 Noggin (500 ng/mL) 的 KSR 培养基培养 11 天,使用 Immunofluorescence 方法检测细胞分化情况。
结果:神经诱导通过 PAX6 的表达来监测,PAX6 是神经直肠真皮分化的早期标志物。与单独使用 Noggin 或 SB-431542 时不到 10% 的 PAX6+ 细胞相比,用 Noggin 和 SB-431542 联合处理显著提高了神经诱导的效率,使其超过总细胞的 80%。[3]
体内活性 方法:为检测体内抗肿瘤活性,将 SB-431542 (10 mg/kg in 20% DMSO/80% corn oil) 腹腔注射给携带小鼠乳腺癌肿瘤 4T1 的 Balb/c 小鼠,每周三次,持续四周。
结果:SB-431542 可显著抑制 4T1 乳腺肿瘤的肺转移。[4]
方法:为研究肌腱损伤的治疗方法,将 SB-431542 (10 mg/kg) 腹腔注射给大面积肩袖撕裂的 C57B/6J 小鼠模型,每天一次,持续二或六周。
结果:SB-431542 抑制 TGF-β1 信号传导可减少纤维化、脂肪浸润和肌肉重量减轻。SB-431542 治疗通过促进纤维/脂肪生成祖细胞 (FAP) 的凋亡,减少了损伤肌肉中 FAP 的数量,FAP 是肩袖肌纤维化和脂肪浸润的重要细胞来源。[5]
激酶实验 Kinase assays were performed with 65 nM GSTALK5 and 184 nM GST-Smad3 in 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 1 mM dithiothreitol, and 3 M ATP. Reactions were incubated with 0.5 μCi of [33P]γATP for 3 h at 30°C. Phosphorylated protein was captured on P-81 paper, washed with 0.5% phosphoric acid, and counted by liquid scintillation. Alternatively, Smad3 or Smad1 protein was also coated onto FlashPlate Sterile Basic Microplates. Kinase assays were then performed in FlashPlates with same assay conditions using either the kinase domain of ALK5 with Smad3 as a substrate or the kinase domain of ALK6 (BMP receptor) with Smad1 as substrate. Plates were washed three times with phosphate buffer and counted by TopCount [2].
细胞实验 A498 cells were seeded at 5,000 to 10,000 cells/well in 96-well plates. The cells were serum-deprived for 24 h and then treated with compounds for 48 h to assess the cellular toxicity. Cell viability is determined by incubating cells for 4 h with XTT labeling and electron coupling reagent. Live cells with active mitochondria produce an orange-colored product, formazan, which is detected using a plate reader at between A450 nm and A500 nm with a reference wavelength greater than 600 nm. The absorbance values correlate with the number of viable cells [2].
动物实验 BALB/c mice received intraperitoneal (i.p.) injections of colon-26 tumor cells. Three days after tumor cell inoculation, SB-431542 (1 μM solution, 100 μl/animal) or vehicle alone was directly injected into the peritoneal cavity. CTL activities were measured by a standard 4 h 51Cr release assay after culturing spleen cells with γ-irradiated tumor cells for five days in the absence of added growth factors. In vitro experiments, cell lysate of HLA-A*2402 positive gastric cancer cell line, OCUM-8, was incubated with human DC cultures for 4 h. After washing extensively, PBMCs obtained from the same volunteer as DCs were incubated for 7 days and measured CTL activity by 51Cr release assay. NK activity was tested using 51Cr release assay against K562 [4].
别名 4-[4-(1,3-苯并二唑-5-基)-5-(2-吡啶基)-1H-咪唑-2-基]-苯酰胺水合物, SB 431542
分子量 384.39
分子式 C22H16N4O3
CAS No. 301836-41-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 38.4 mg/mL (100 mM)

Ethanol: 3.8 mg/mL (10 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.6015 mL 13.0076 mL 26.0152 mL 65.0381 mL
5 mM 0.5203 mL 2.6015 mL 5.203 mL 13.0076 mL
10 mM 0.2602 mL 1.3008 mL 2.6015 mL 6.5038 mL
DMSO 20 mM 0.1301 mL 0.6504 mL 1.3008 mL 3.2519 mL
50 mM 0.052 mL 0.2602 mL 0.5203 mL 1.3008 mL
100 mM 0.026 mL 0.1301 mL 0.2602 mL 0.6504 mL

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TargetMol Library Books参考文献

1. Halder SK, et al. A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Neoplasia. 2005 May;7(5):509-21. 2. Hjelmeland MD, et al. SB-431542, a small molecule transforming growth factor-beta-receptor antagonist, inhibits human glioma cell line proliferation and motility. Mol Cancer Ther. 2004 Jun;3(6):737-45. 3. Chambers SM, et al. Highly efficient neural conversion of human ES and iPS cells by dual inhibition of SMAD signaling. Nat Biotechnol. 2009 Mar;27(3):275-80. doi: 10.1038/nbt.1529. Epub 2009 Mar 1. Erratum in: Nat Biotechnol. 2009 May;27(5):485. 4. 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. 5. Davies MR, et al. TGF-β Small Molecule Inhibitor SB431542 Reduces Rotator Cuff Muscle Fibrosis and Fatty Infiltration By Promoting Fibro/Adipogenic Progenitor Apoptosis. PLoS One. 2016 May 17;11(5):e0155486. 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. 7. Duan F, Huang R, Zhang F, et al. Biphasic modulation of insulin signaling enables highly efficient hematopoietic differentiation from human pluripotent stem cells[J]. Stem cell research & therapy. 2018 Jul 27;9(1):205. 8. Xiong, Yanlu, et al. TFAP2A potentiates lung adenocarcinoma metastasis by a novel miR-16 family/TFAP2A/PSG9/TGF-β signaling pathway. . Cell Death & Disease . 12.4 (2021): 1-13. 9. Chen F, Gao Q, Wei A, et al. Histone deacetylase 3 aberration inhibits Klotho transcription and promotes renal fibrosis[J]. Cell Death & Differentiation. 2020: 1-12.

TargetMol Library Books文献引用

1. Chen X, Wang P, Qiu H, et al. Integrative epigenomic and transcriptomic analysis reveals the requirement of JUNB for hematopoietic fate induction. Nature Communications. 2022, 13(1): 1-16 2. Duan F, Huang R, Zhang F, et al. Biphasic modulation of insulin signaling enables highly efficient hematopoietic differentiation from human pluripotent stem cells. Stem Cell Research & Therapy. 2018 Jul 27;9(1):205 3. Bao, Shixiang, et al. TGF-β1 Induces Immune Escape by Enhancing PD-1 and CTLA-4 Expression on T Lymphocytes in Hepatocellular Carcinoma. Frontiers in Oncology. 11 (2021): 2516. 4. Bao, Shixiang, et al. TGF-β1 Induces Immune Escape by Enhancing PD-1 and CTLA-4 Expression on T Lymphocytes in Hepatocellular Carcinoma. Frontiers in Oncology. 11 (2021): 2516. 5. Bao, Shixiang, et al. TGF-β1 Induces Immune Escape by Enhancing PD-1 and CTLA-4 Expression on T Lymphocytes in Hepatocellular Carcinoma. Frontiers in Oncology. 11 (2021): 2516. 6. Fu J, Jiang L, Yu B, et al. Generation of a Human iPSC Line CIBi010-A with a Reporter for ASGR1 Using CRISPR/Cas9. Stem Cell Research. 2022: 102800 7. Liu S, Yan X, Guo J, et al.Periodontal ligament‐associated protein‐1 knockout mice regulate the differentiation of osteoclasts and osteoblasts through TGF‐β1/Smad signaling pathway.Journal of Cellular Physiology.2023 8. Ying J, Wang P, Jin X, et al.TGF-β1 Mediates the EndoMt in High Glucose-Treated Human Retinal Microvascular Endothelial Cells.Seminars in Ophthalmology. Taylor & Francis.2024: 1-8.
6-Demethoxytangeretin Repotrectinib AZ12601011 D4476 A 83-01 sodium salt ALK inhibitor 1 MS4077 CEP-28122

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 高选择性抑制剂库 抑制剂库 抗癌活性化合物库 TGF-β/Smad靶点化合物库 激酶抑制剂库 抗胰腺癌化合物库 抗乳腺癌化合物库 血管生成库 已知活性化合物库

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Keywords

SB-431542 301836-41-9 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad Transforming growth factor beta receptors inhibit 4-[4-(1,3-苯并二唑-5-基)-5-(2-吡啶基)-1H-咪唑-2-基]-苯酰胺水合物 SB 431542 TGF-β Receptor SB431542 Inhibitor inhibitor

 

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