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18438616290
簡要描述：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.
產(chǎn)品型號：abs810374廠商性質(zhì)：生產(chǎn)廠家更新時(shí)間：2025-11-11訪 問 量：1064產(chǎn)品分類
Product Category詳細(xì)介紹
| 品牌 | absin | CAS | 356559-20-1 |
|---|---|---|---|
| 分子式 | C21H21N5 | 純度 | >98% |
| 分子量 | 343.42 | 貨號 | abs810374 |
| 規(guī)格 | 2mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | SB-525334；SB 525334；TGF-β RI Kinase Inhi | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
SB525334
| 產(chǎn)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. |
| 純度 | >98% |
| 儲(chǔ)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 | |
| 別名 | SB-525334；SB 525334；TGF-β RI Kinase Inhibitor VIII |
| 外觀 | 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 | |
| 靶點(diǎn) | TGFβR1(ALK5) |
| In vitro(體外研究) | 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(體內(nèi)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. |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | CancerCancer Metabolism Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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