83-01(DMSO溶液

TGFβRI/ALK5 选择性抑制剂
  • 10mM in DMSO
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
A408570-1ml
1ml 现货 Stock Image
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Compound libraries (12326)

基本描述

英文别名 1H-​Pyrazole-​1-​carbothioamide, 3-​(6-​methyl-​2-​pyridinyl)​-​N-​phenyl-​4-​(4-​quinolinyl)​-
规格或纯度 10mM in DMSO
英文名称 A-83-01
生化机理 A-83-01 是 TGF-β I 型受体(ALK5-TD)的强效抑制剂,IC50 为 12 nM。A-83-01 还能抑制活化素/结节 I 型受体(ALK4-TD)和结节 I 型受体(ALK7-TD)诱导的转录,IC50 分别为 45 nM 和 7.5 nM。
储存温度 -80℃储存
运输条件 超低温冰袋运输
产品介绍

A 83-01 是一种有效的 TGF-β I 型受体 ALK5,ALK4 和 ALK7 的抑制剂,能够抑制 ALK5,ALK4 和 ALK7 诱导的转录,IC50 值分别为 12 nM,45 nM 和 7.5 nM。

Information

A-83-01 is a potent inhibitor ofTGF-β type I receptor (ALK5-TD)with IC50 of 12 nM. A-83-01 also inhibits the transcription induced byactivin/nodal type I receptor (ALK4-TD)andnodal type I receptor (ALK7-TD)with IC50 of 45 nM and 7.5 nM, respectively.Solut
In vitro

A-83-01 inhibits the transcriptional activity induced by TGF-β type I receptor ALK-5 and that by activin type IB receptor ALK-4 and nodal type I receptor ALK-7, the kinase domains of which are structurally highly related to those of ALK-5. A-83-01 is potent in the inhibition of ALK5 and also prevents phosphorylation of Smad2/3 and the growth inhibition induced by TGF-β.

In vivo

A83-01 treatment significantly increases the number of Nkx2.5+ cardiomyoblasts at baseline and after myocardial injury, resulting in an increase in newly formed cardiomyocytes. A83-01 treatment significantly improves ventricular elastance and stroke work, leading to improved contractility after injury.
Cell Data

cell lines:

Concentrations:1 μM

Incubation Time:1 h

Powder Purity:

产品属性

IC50 ALK5, IC50: 12 nM

名称和识别符

Canonical SMILES CC1=CC=CC(=N1)C2=N[N](C=C2C3=CC=NC4=CC=CC=C34)C(=S)NC5=CC=CC=C5
分子量 421.52

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 47 mg/mL (197.28 mM);    

安全和危险性(GHS)

质量标准

Concentration
Proton NMR spectrum Conforms to Structure

质检证书(CoA,COO,BSE/TSE 和分析图谱)

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