全国服务咨询热线：
18438616290
18438616290
产品分类
Product Category详细介绍
| 品牌 | absin | CAS | 356559-20-1 |
|---|---|---|---|
| 分子式 | C21H21N5 | 纯度 | >98% |
| 分子量 | 343.42 | 货号 | abs810374 |
| 规格 | 2mg | 供货周期 | 现货 |
| 主要用途 | SB-525334；SB 525334；TGF-β RI Kinase Inhi | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
SB525334
| 产品描述 | |
| 描述 | SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | SB-525334；SB 525334；TGF-β RI Kinase Inhibitor VIII |
| 外观 | yellow Powder |
| 可溶性/溶解性 | 1eq. HCl : 34.3 mg/mL (100 mM) DMSO : 34.3 mg/mL (100 mM) |
| 生物活性 | |
| 靶点 | TGFβR1(ALK5) |
| In vitro(体外研究) | SB 525334 shows no inhibition in the enzymes ALK2, 3, and 6, with IC50 values > 10 μM. SB 525334 blocks phosphorylation induced by TGF-β1 and nuclear translocation of Smad2/3 in renal proximal tubule cells. SB 525334 also inhibits the increased mRNA expression levels of plasminogen activator inhibitor-1 (PAI-1) and procollagen α1(I) induced by TGF-β1 in A498 renal epithelial carcinoma cells at 1 μM). SB 525334 (1 μM) attenuates the heightened sensitivity to TGF-β1 exhibited by pulmonary artery smooth muscle cells (PASMCs) from patients with familial forms of idiopathic pulmonary arterial hypertension (PAH). |
| In vivo(体内研究) | SB 525334 (10 mg/kg/day) decreases the renal mRNA levels of PAI-1, procollagen α1(I), and procollagen α1(III) in a nephritis-induced renal fibrosis rat model. Furthermore, PAN-induced proteinuria is significantly inhibited by SB 525334 (10 mg/kg/day). SB 525334 may also be efficacious in mesenchymal tumors. SB 525334 (10 mg/kg/day) significantly decreases uterine mesenchymal tumor incidence, multiplicity, and size in Eker rats. SB 525334 significantly reverses pulmonary arterial pressure and inhibits right ventricular hypertrophy in a rat model of PAH. This is revealed by a significant reduction in pulmonary arteriole muscularization induced by monocrotaline (used to induce PAH) after treatment with SB 525334 (3 or 30 mg/kg). In a Bleomycin-induced pulmonary fibrosis mice model, SB 525334 (10 mg/kg or 30 mg/kg) attenuates the histopathological alterations in the lung, and significantly decreased mRNA expression of Type I and III procollagen and fibronectin. SB 525334 also attenuates Smad2/3 nuclear translocation, myofibroblast proliferation, deposition of Type I collagen, and decreases CTGF-expressing cells. |
| 研究领域 | |
| 研究领域 | CancerCancer Metabolism Drug DiscoverySmall Molecule DrugLead Compound Discovery |
产品咨询
地址：上海市浦东新区新浩路58号申江科创园18栋
邮箱：lanwu@univ-bio.com
传真：