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A 83-01 sodium salt
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
A 83-01 sodium salt图片
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
A potent inhibitor of TGF-β type I receptor ALK5 kinase
Canonical SMILESS=C(N1N=C(C2=NC(C)=CC=C2)C(C3=CC=NC4=CC=CC=C34)=C1)NC5=CC=CC=C5.[Na+]
分子式C25H19N5NaS
分子量444.51
溶解度DMSO: 100 mg/mL (224.97 mM); Water:< 0.1 mg/mL (insoluble)
储存条件4°C, protect from light *Product is unstable in the solution state, it is recommended that you use it now and use it immediately
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively. IC50: 12 nM (ALK5, cell-based), 45 nM (ALK4 cell-based), 7.5 nM (ALK7 cell-based)[1]

A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, reduces the level of ALK-5-induced transcription with an IC50 of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC50s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10 µM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 µM. A 83-01 (1-10 µM) inhibits TGF-β-induced Smad activation in HaCaT cells[1]. A 83-01 (1 µM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation[2].

A 83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances[2]. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells[3].

[1]. Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005 Nov;96(11):791-800. [2]. Yamamura S, et al. The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. Int J Cancer. 2012 Jan 1;130(1):20-8. [3]. Taniguchi Y, et al. Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13.