RepSox | TGF-beta/Smad | AmBeed-信号通路专用抑制剂

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RepSox {[allProObj[0].p_purity_real_show]}

货号：A158647

RepSox (E-616452)是一种有效且选择性的TGF-β-RI/ALK5抑制剂。

RepSox 化学结构
CAS号：446859-33-2

RepSox 3D分子结构
CAS号：446859-33-2

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RepSox 纯度/质量文件产品仅供科研

货号：A158647 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

转化生长因子-β 亚型比较

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		99%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

RepSox 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]

RepSox 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

RepSox 动物研究

Dose	Mice: 8.6 mg/kg (p.o.)
Administration	p.o.

RepSox 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

RepSox 实验方案

计算器

存储液制备

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

RepSox 技术信息

CAS号	446859-33-2
分子式	C₁₇H₁₃N₅
分子量	287.319

别名
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

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

RepSox {[allProObj[0].p_purity_real_show]}

RepSox 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

RepSox 质控信息

RepSox 生物活性

RepSox 细胞研究

RepSox 动物研究

RepSox 参考文献

RepSox 实验方案

RepSox 技术信息

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RepSox {[allProObj[0].p_purity_real_show]}

RepSox 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

RepSox 质控信息

RepSox 生物活性

RepSox 细胞研究

RepSox 动物研究

RepSox 参考文献

RepSox 实验方案

RepSox 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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热门区域

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C

F

G

H

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RepSox 纯度/质量文件产品仅供科研