SB-525334

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Chemical Structure| 356559-20-1 同义名 : TGF-β RI Kinase Inhibitor VIII
CAS号 : 356559-20-1
货号 : A187949
分子式 : C21H21N5
纯度 : 99%+
分子量 : 343.425
MDL号 : MFCD11045307
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(305.74 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • TGFβRI/ALK5

    TGFβR1(ALK5), IC50:14.3 nM
描述 The TGF-β pathway regulates a wide variety of cellular processes in many different cell types and biological contexts. There are three identified TGF receptor ligands, TGF-β1, 2, and 3. Activated TGF-β ligands can interact with TGF-β type II receptors (TβRII), then recruit and phosphorylate the TGF-β type I receptors (also called as TβRI or ALK5). In turn, activated TβRI phosphorylates SMAD2 and SMAD3 at C-terminal serine residues. Following that, phosphorylated SMAD and SMAD3 assemble into heterodimeric and trimeric complexes with SMAD4. Then the trimeric complex translocate into the nucleus and regulate the expression of TGF-β target genes[1]. SB-525334 is an ALK5 inhibitor with IC50 value of 14.3 nM, with modest potent to ALK4 with an IC50 value of 58.5 nM (measured by GST-ALKs kinase assay). Addition of 1 μM SB-525334 reduced TGF-β1-induced Smad2 and Smad3 nuclear localization back to the control levels in RPTE cells[2]. SB-525334 on concentration of 0.5 - 2 μM can inhibit p-SMAD2 in dose-dependent manner in ELT-3 cells[3]. SB525334, 30 mg/kg, given twice daily by oral gavage for 2 weeks can attenuate f bleomycin-induced lung fibrosis in mice[4].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
AsPC1 0-10 μM Cell Viability Assay 72 h efficiently reduces the viability with gemcitabine 22399597
ELT-3 0.5/1.0/2.0 μM Function Assay 1 h inhibits TGF-β signaling in leiomyomas 17505012
HUVECs 10 μM Function Assay 24/48/72 h leads to a disruption of the HUVEC monolayer after 72 hr 23968981
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.91mL

0.58mL

0.29mL

14.56mL

2.91mL

1.46mL

29.12mL

5.82mL

2.91mL
参考文献

[1]Colak S, Ten Dijke P, et al. Targeting TGF-β Signaling in Cancer. Trends Cancer. 2017 Jan;3(1):56-71.

[2]Grygielko ET, Martin WM, 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. Epub 2005 Mar 15.

[3]Laping NJ, Everitt JI, et al. Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats. Clin Cancer Res. 2007 May 15;13(10):3087-99.

[4]Scotton CJ, Hayes B, et al. Ex vivo micro-computed tomography analysis of bleomycin-induced lung fibrosis for preclinical drug evaluation. Eur Respir J. 2013 Dec;42(6):1633-45.