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SB-505124

SB-505124

产品编号 T2462   CAS 694433-59-5

SB505124 是TGF-βI 型受体 (ALK4,ALK5,ALK7) 的选择性抑制剂,能够抑制 ALK4 (IC50:129 nM),ALK5 (IC50:47 nM),对 ALK1,2,3 或 6 无影响。

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SB-505124 Chemical Structure
SB-505124, CAS 694433-59-5
规格 价格/CNY 货期 数量
1 mg ¥ 258 现货
2 mg ¥ 367 现货
5 mg ¥ 576 现货
10 mg ¥ 927 现货
25 mg ¥ 1,690 现货
50 mg ¥ 2,870 现货
100 mg ¥ 3,990 现货
500 mg ¥ 8,730 现货
1 mL * 10 mM (in DMSO) ¥ 965 现货
其他形式的 SB-505124:
产品目录号及名称: SB-505124 (T2462)
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选择批次  
纯度: 99.92%
纯度: 99%
纯度: 98.74%
纯度: 97.88%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5.
靶点活性 ALK4:129 nM, ALK5:47 nM
体外活性 在兔GFS模型中,SB505124降低了GFS手术部位的眼内压(IOP)水平并减少了结膜下细胞浸润和瘢痕形成.在他克莫司(TAC)治疗的小鼠和FK12EC KO小鼠中,SB505124抑制内皮细胞TGF-β受体的活化和肾小动脉玻璃样变性的诱导.
体内活性 SB505124被鉴定为ALK4和ALK5的可逆ATP竞争性和选择性ALK抑制剂。SB-505124抑制紧密相关的ALK4,IC50为129 nM,选择性比作用于ALK5低2.5倍。SB-505124浓度高达10 μM时也不抑制ALK2。SB-505124抑制COS-1细胞内源性Smad2磷酸化。ALK4和ALK5激活Smad1和Smad2,加入SB-505124抑制激活。SB-505124作用于HepG2人类肝癌细胞,C2C12小鼠成肌细胞和Mv1Lu水貂肺细胞,浓度依赖性抑制转化生长因子-β诱导的Smad2磷酸化。SB-505124有效抑制转化生长因子-β和活化素诱导CAGA12-荧光素酶和ARE-荧光素酶受体结构的活力,这种作用存在浓度依赖性。在人脐静脉内皮细胞(HUVEC)中,SB505124(500 nM)阻断TGF-β1对F-actin组装的影响,并阻止TGF-β诱导的ROS产生。
激酶实验 In Vitro Protein Kinase Assay : Kinase assays are performed as described by Laping et al., 2002 using the kinase domain of ALK5 and full-length N-terminal fused GST-Smad3. Kinase assays are performed with 65 nM GST-ALK5 and 184 nM GST-Smad3 in 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 1 mM dithiothreitol, and 3 μM ATP. Reactions are incubated with 0.5 μCi of [33P]γATP for 3 hours at 30 °C. Phosphorylated protein is captured on P-81 paper , washed with 0.5% phosphoric acid, and counted by liquid scintillation. Alternatively, Smad3 or Smad1 protein is also coated onto FlashPlate Sterile Basic Microplates. Kinase assays are then performed in FlashPlates with same assay conditions using either the kinase domain of ALK5 with Smad3 as substrate or the kinase domain of ALK6 (BMP receptor) with Smad1 as substrate. Plates are washed three times with phosphate buffer and counted by TopCount.
细胞实验 Cell viability is measured as described by Laping et al., 2002 or by using the modified tetrazolium salt WST-1. XTT assay: The cells are serum-deprived for 24 hours and then treated with SB505124 for 48 hours to assess the cellular toxicity. Cell viability is determined by incubating cells for 4 hours with XTT labeling and electron coupling reagent according to the manufacturer's directions. 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. Modified tetrazolium salt WST-1: Approximately 2000 cells are seeded in 96-well dishes in 100 μL of 0.2% FBS phenol red-free media overnight. The cells are treated with 50 μL of SB505124 (to achieve the final concentrations indicated) for 30 minutes before being treated with or without TGF-β1 and TNF-α to a final volume of 200 μL. Cell growth is measured at the indicated time points by incubating each well with 10 μL of WST-1 for 3 hours at 37 °C. Metabolically active cells cleave WST-1 to water-soluble formazan, which is directly quantitated with an enzyme-linked immunosorbent assay plate reader. Each experiment is done at least twice, and treatment for each cell line is done in triplicate.(Only for Reference)
分子量 335.4
分子式 C20H21N3O2
CAS No. 694433-59-5

存储

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

溶解度

DMSO: 33.5 mg/mL (100 mM)

1eq. HCl: 33.5 mg/mL (100 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 / 1eq. HCl 1 mM 2.9815 mL 14.9076 mL 29.8151 mL 74.5379 mL
5 mM 0.5963 mL 2.9815 mL 5.963 mL 14.9076 mL
10 mM 0.2982 mL 1.4908 mL 2.9815 mL 7.4538 mL
20 mM 0.1491 mL 0.7454 mL 1.4908 mL 3.7269 mL
50 mM 0.0596 mL 0.2982 mL 0.5963 mL 1.4908 mL
100 mM 0.0298 mL 0.1491 mL 0.2982 mL 0.7454 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. DaCosta Byfield S, et al. Mol Pharmacol. 2004, 65(3), 744-752. 2. Hu T, et al. Am J Physiol Renal Physiol. 2005, 289(4), F816-825. 3. Misumi S, et al. Eur J Neurosci. 2008, 28(6), 1049-1059. 4. Goto N, et al. Cancer Sci. 2011, 102(8), 1501-1508. 5. Sapitro J, et al. Mol Vis. 2010 ,16, 1880-1892. 6. Marini KD, et al. Inhibition of activin signaling in lung adenocarcinoma increases the therapeutic index of platinum chemotherapy. Sci Transl Med. 2018 Jul 25;10(451). pii: eaat3504. 7. Kalli M, Mpekris F, Wong C K, et al. Activin A signaling regulates IL13Rα2 expression to promote breast cancer metastasis[J]. Frontiers in oncology. 2019 Feb 5;9:32.

文献引用

1. Kalli M, Mpekris F, Wong C K, et al. Activin A signaling regulates IL13Rα2 expression to promote breast cancer metastasis. Frontiers in Oncology. 2019 Feb 5;9:32 2. Liu S, Yu X, Guo Q, et al.Periodontal ligament‐associated protein‐1 promotes osteoclastogenesis in mice by modulating TGF‐β1/Smad1 pathway.Journal of Periodontology.2023
Brigatinib 6-Demethoxytangeretin K02288 Vactosertib Hydrochloride A 83-01 sodium salt D4476 Ceritinib dihydrochloride AZ7550

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 抗癌活性化合物库 TGF-β/Smad靶点化合物库 抗纤维化化合物库 抗乳腺癌化合物库 抗肥胖化合物库 抗肝癌化合物库 癌细胞分化化合物库 干细胞分化化合物库 抗心血管疾病化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

SB-505124 694433-59-5 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad SB505124 SB 505124 Transforming growth factor beta receptors TGF-β Receptor Inhibitor inhibit inhibitor

 

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