|2-(3-(6-甲基吡啶-2-基)-1H-吡唑-4-基)-1,5-萘啶|CsnPharm

CAS No.: 446859-33-2

2-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine Catalog No. CSN12299

Synonyms: E-616452;SJN 2511;ALK5 Inhibitor II

RepSox is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 TGFβR1

IC50:23nM
描述TGFβ family members, including TGFβs and BMPs, play a key role during embryonic development, in processes of cell differentiation^[2]. RepSox is a selective inhibitor of TGF-β type I receptor (also called as TβRI or ALK5) with IC50 value of 4nM (measured by ALK5 autophosphorylation assay)^[1]. RepSox is mainly used in cell reprogramming and differentiation as following: 1. direct reprogramming of mouse fibroblasts into cardiomyocytes, combined with CHIR99021, Forskolin, VPA, Parnate, TTNPB and DZnep^[3]. 2. replaces Sox2 in reprogramming by inducing Nanog^[4].
作用机制RepSox can bound to the ATP binding site of the kinase domain of ALK5.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
baculovirus/Sf9 cells	-	Function assay	-	Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells, IC50=4 nM	15317461
HepG2 cells	-	Function assay	-	Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells, IC50=10 nM	15317461

动物研究
剂量
Mice: 8.6 mg/kg (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 8.6 mg/kg (p.o.)
给药途径	p.o.

[1] Gellibert F, Woolven J, et al. Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. J Med Chem. 2004 Aug 26;47(18):4494-506.
[2] Puc¨¦at M, et al. TGFbeta in the differentiation of embryonic stem cells. Cardiovasc Res. 2007 May 1;74(2):256-61. Epub 2006 Dec 16.
[3] Fu Y, Huang C, et al. Direct reprogramming of mouse fibroblasts into cardiomyocytes with chemical cocktails. Cell Res. 2015 Sep;25(9):1013-24.
[4] Ichida JK, Blanchard J, et al. A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog. Cell Stem Cell. 2009 Nov 6;5(5):491-503

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
- 3.4805 mL
- 17.4023 mL
- 34.8046 mL
- 5 mM
- 0.6961 mL
- 3.4805 mL
- 6.9609 mL
- 10 mM
- 0.3480 mL
- 1.7402 mL
- 3.4805 mL

技术信息

CAS号

446859-33-2

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

C17H13N5

运输

蓝冰

分子量

287.32

别名

E-616452;SJN 2511;ALK5 Inhibitor II

溶解度

DMSO	100.0 mg/mL (348.0 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+water	2 mg/mL	clear
PO	0.5% CMC-Na	70 mg/mL	suspension

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2-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine Catalog No. CSN12299

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