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CAS No.: 356559-20-1

SB-525334 Catalog No. CSN13435

Synonyms: TGF-β RI Kinase Inhibitor VIII

SB-525334 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.

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生物活性

实验方案

技术信息

生物活性

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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动物研究
剂量
Rat^[2] (p.o): min = 1 mg/kg, max = 10 mg/kg

给药途径
p.o.

动物药代数据
Animal Rats^[2]
Dose 10 mg/kg
Administration p.o.
T_1/2 115 min
CL 1 ml/min/100 g
F 0.87
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9118 mL
- 14.5592 mL
- 29.1184 mL
- 5 mM
- 0.5824 mL
- 2.9118 mL
- 5.8237 mL
- 10 mM
- 0.2912 mL
- 1.4559 mL
- 2.9118 mL

技术信息

CAS号

356559-20-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H21N5

运输

蓝冰

分子量

343.42

别名

TGF-β RI Kinase Inhibitor VIII

溶解度

DMSO	68.0 mg/mL (198.0 mM)
Water	Insoluble
Ethanol	68.0 mg/mL (198.0 mM)

动物实验配方

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