452342-67-5|GW788388|CsnPharm

CAS No.: 452342-67-5

GW788388 Catalog No. CSN13159

Synonyms: GW788388

GW788388 is a selective ALK5 inhibitor with IC50 of 18 nM and also inhibits TGF-β type II receptor and activin type II receptor.

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技术信息

生物活性

描述Transforming growth factor β (TGF-β) type I receptor (ALK5) is a transmembrane serine/threonine kinase. ALK5 forms a heteromeric complex with type II TGF-beta receptors when bound to TGF-beta, transducing the TGF-beta signal from the cell surface to the cytoplasm. Thus, ALK5 participates in regulation of physiological and pathological processes including cell cycle arrest in epithelial and hematopoietic cells, control of mesenchymal cell proliferation and differentiation, wound healing, extracellular matrix production, immunosuppression and carcinogenesis. GW788388 is an ALK5 kinase inhibitor with IC₅₀ of 18 nM^[3]. NMuMG and MDA-MB-231 cells were treated with GW788388 at the concentrations of 1 μM, 5 μM and 10 μM or 2.5 μM, 5 μM and 10 μM, respectively，in the presence of TGF-β for 1 h and the results showed that GW788388 inhibited TGF-β induced Smad2 phosphorylation in a dose-dependent manner in both cell lines^[4]. In a rat model of chemically induced renal fibrosis, GW788388 administration at the doses of 3 mg/kg or 10 mg/kg u.i.d. significantly decreased relative collagen IA1 mRNA levels^[3]. In a renal fibrosis model using db/db mice, GW788388 given orally at the dose of 2 mg/kg/day for 5 weeks significantly reduced renal fibrosis and decreased the mRNA levels of key mediators of extracellular matrix deposition in kidneys^[4]. In a mouse model of bleomycin-induced dermal fibrosis, GW788388 given i.p. at the dose of 2 mg/kg/day prevented the fibrotic response^[5].
作用机制GW788388 is an ATP competitive inhibitor of the kinase domain of ALK5^[4].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HEK293 cells	-	Function assay	-	Inhibition of TGF-beta1 signaling in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX after 16 hrs by luciferase reporter gene assay, IC50=0.446 μM	21783359
HepG2 cells	-	Function assay	-	Inhibition of TGF beta-induced transcription of firefly luciferase reporter gene in HepG2 cells, IC50=0.093 μM	16570917

参考文献

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
- 2.3503 mL
- 11.7514 mL
- 23.5029 mL
- 5 mM
- 0.4701 mL
- 2.3503 mL
- 4.7006 mL
- 10 mM
- 0.2350 mL
- 1.1751 mL
- 2.3503 mL

技术信息

CAS号

452342-67-5

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

C25H23N5O2

运输

蓝冰

分子量

425.48

别名

GW788388

溶解度

DMSO	55.0 mg/mL (129.3 mM) warming
Water	insoluble

动物实验配方

5%DMSO+40%PEG400+5% tween80+H2O

5 mg/mL

clear

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