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SB 525334

SB 525334

产品编号 T1763   CAS 356559-20-1
别名: SB525334

SB525334是转化生长因子β1受体 (ALK5) 选择性抑制剂,IC50=14.3 nM。

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SB 525334 Chemical Structure
SB 525334, CAS 356559-20-1
规格 价格/CNY 货期 数量
5 mg ¥ 398 现货
10 mg ¥ 685 现货
25 mg ¥ 1,456 现货
50 mg ¥ 2,590 现货
100 mg ¥ 3,996 现货
200 mg ¥ 4,580 现货
1 mL * 10 mM (in DMSO) ¥ 453 现货
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: SB 525334 (T1763)
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选择批次  
纯度: 99.86%
纯度: 99%
纯度: 98.9%
纯度: 98.39%
纯度: 98%
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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-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM).
靶点活性 ALK5:14.3 nM (cell free), ALK4:58.5 nM
体外活性 SB-525334 (1 μM) blocked TGF-beta1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells and inhibited TGF-beta1-induced increases in plasminogen activator inhibitor-1 (PAI-1) and procollagen alpha1(I) mRNA expression in A498 renal epithelial carcinoma cells [1]. The combination with SB525334 significantly augmented the cytotoxicity of gemcitabine in both parental and gemcitabine-resistant pancreatic cancer cells. SB525334 significantly increased apoptotic cell death in gemcitabine-resistant cells [2].
体内活性 Orally administered doses of 1, 3, or 10 mg/kg/day SB-525334 for 11 days produced statistically significant reductions in renal PAI-1 mRNA [1]. SB-525334 (10 mg/kg or 30 mg/kg) was orally administered at twice a day. Lungs were isolated 5, 7, 9 and 14 days after Bleomycin (BLM) treatment. BLM treatment led to significant pulmonary fibrotic changes accompanied by significant upregulation of ECM mRNA expressions, Smad2/3 nuclear translocation, CTGF expression, myofibroblast proliferation and type I collagen deposition. SB-525334 treatment attenuated the histopathological alterations in the lung, and significantly decreased the type I and III procollagen and fibronectin mRNA expression [3].
激酶实验 To determine the potency of the ALK5 inhibitor SB-525334 at the enzyme level, purified GST-tagged kinase domain of ALK5 was incubated with purified GST-tagged full-length Smad3 in the presence of 33P-γATP and different concentrations of SB525334. The readout is radioactively labeled Smad3. To determine the selectivity of SB-525334, purified GST-tagged kinase domain of ALK2 and ALK4 were incubated with GST-tagged full-length Smad1 and Smad3, respectively, in the presence of different concentrations of SB-525334 (n=3). IC50 value determinations were calculated with GraphPad software using a sigmoidal dose-response curve [1].
细胞实验 RPTE cells were seeded on microscope slides. The following day, the cells were starved by removal of epidermal growth factor and serum for 24 h prior to dosing. Cells were dosed with 10 ng/ml TGF- 1 or 1 M SB-525334 or a combination of both. Slides were pretreated with SB-525334 or starve media for 3 h prior to a 1-h incubation at 37°C with TGF- 1 or starve media. The cells were then fixed for 15 min in 4% ice-cold paraformaldehyde. The cells were permeabilized for 10 min in 0.3% Triton X-100/PBS at room temperature. The slides were incubated for 30 min in a blocking solution containing 0.3% bovine serum albumin, 10% FBS, 0.3% Triton X-100/PBS, and 5% milk in PBS. A 1:200 dilution of primary mouse anti-Smad2/3 antibody was applied to each slide for overnight incubation. A 1:200 dilution of anti-mouse IgG fluorescein secondary antibody was applied to each slide for 30 min at room temperature. The slides were then viewed using an argon blue 488 nM laser in a confocal microscope. Nuclear signal intensity was analyzed using 1D Image Analysis software. The relative intensity was determined by the mean intensity of the nucleus and expressed as percent control [1].
动物实验 To identify the optimal treatment length for puromycin aminonucleoside's effect on extracellular matrix in the kidney, 18 Sprague-Dawley (SD) rats (200 –250 g) were injected with 15 mg/100 g of puromycin aminonucleoside in 0.9% saline or sham 0.9% saline only intraperitoneally. Animals were sacrificed at 24 h (n = 3+2 control), day 4 (n=3), day 8 (n = 3), day 10 (n = 3), day 15 (n = 2), and day 20 (n = 2). A 24-h urine collection and plasma sample were taken at 9:00 AM everyday. Urine and plasma chemistry were measured at GlaxoSmithKline Laboratories Animal Science using an Olympus clinical analyzer. Proteinuria was measured as a concentration (mg/deciliter) and then converted to total protein excreted over a 24-h period using urine flow (mL/24 h). The creatinine clearance was calculated by multiplying urine creatinine levels (mg/mL) by urine flow (mg/mL/100 g b.wt.) and then dividing that product by plasma creatinine (mg/mL). To determine the effect of SB-525334 on renal disease in the PAN model, SD rats were pretreated by oral gavage with 1, 3, or 10 mg/kg/day of SB-525334 once a day. The following day, PAN was injected at 15 mg/100 g to the appropriate rats. Treatment groups continued to receive SB-525334. Ten days after PAN injection the rats were sacrificed, and blood, urine, and kidneys were collected at the termination point for analysis [1].
别名 SB525334
分子量 343.42
分子式 C21H21N5
CAS No. 356559-20-1

存储

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

溶解度

DMSO: 34.3 mg/mL (100 mM)

1eq. HCl: 34.3 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 2.9119 mL 14.5594 mL 29.1189 mL 72.7972 mL
5 mM 0.5824 mL 2.9119 mL 5.8238 mL 14.5594 mL
10 mM 0.2912 mL 1.4559 mL 2.9119 mL 7.2797 mL
20 mM 0.1456 mL 0.728 mL 1.4559 mL 3.6399 mL
50 mM 0.0582 mL 0.2912 mL 0.5824 mL 1.4559 mL
100 mM 0.0291 mL 0.1456 mL 0.2912 mL 0.728 mL

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TargetMol Library Books参考文献

1. Grygielko ET, et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J Pharmacol Exp Ther. 2005 Jun;313(3):943-51. 2. Kim YJ, et al. Transforming growth factor beta receptor I inhibitor sensitizes drug-resistant pancreatic cancer cells to gemcitabine. Anticancer Res. 2012 Mar;32(3):799-806. 3. Higashiyama H, et al. Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis. Exp Mol Pathol. 2007 Aug;83(1):39-46.

TargetMol Library Books文献引用

1. Peng H, Shen J, Long X, et al. Local Release of TGF‐β Inhibitor Modulates Tumor‐Associated Neutrophils and Enhances Pancreatic Cancer Response to Combined Irreversible Electroporation and Immunotherapy, Local Release of TGF‐β Inhibitor Modulates Tumor‐Associated Neutrophils and Enhances Pancreatic Cancer Response to Combined Irreversible Electroporation and Immunotherapy. Advanced Science. 2022: 2105240
X-376 EW-7195 EML4-ALK kinase inhibitor 1 Entrectinib MS4078 ALK inhibitor 2 MS4077 Vactosertib

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 激酶抑制剂库 TGF-β/Smad靶点化合物库 膜蛋白靶向化合物库 酪氨酸激酶分子库 抗肝癌化合物库 抗纤维化化合物库 抗癌化合物库 NO PAINS 化合物库 抗肥胖化合物库

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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。

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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 525334 356559-20-1 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad SB525334 inhibit Inhibitor TGF-β Receptor Transforming growth factor beta receptors SB-525334 inhibitor

 

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