RepSox

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Chemical Structure| 446859-33-2 同义名 : -
CAS号 : 446859-33-2
货号 : A158647
分子式 : C17H13N5
纯度 : 98%
分子量 : 287.319
MDL号 : MFCD09037561
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: 35 mg/mL(121.82 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：

IP 2% DMSO+water 2 mg/mL clear

PO 0.5% CMC-Na 70 mg/mL suspension

生物活性
靶点

  • TGFβRI/ALK5

    TGFβR1(ALK5), IC50:4 nM
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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.48mL

0.70mL

0.35mL

17.40mL

3.48mL

1.74mL

34.80mL

6.96mL

3.48mL
参考文献

[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