ITD-1

ITD-1CAS号: 1099644-42-4分子式: C27H29NO3分子量: 415.52描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)

产品描述
描述
ITD-1 is an inducer of TGF_beta_ type II receptor degradation-1, is a potent and highly selective TGF_beta_ pathway inhibitor (IC50 = 0.85 uM).
纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
ITD 1
外观
Light yellow solid
可溶性/溶解性
DMSO : 28 mg/mL (67.39 mM)
生物活性
靶点
TGF-(beta) Receptor
In vitro(体外研究)
ITD-1 potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2, and only minimally in response to Activin A. HEK293T cells are transfected with a Smad4 response element driving luciferase (SBE4-Luc) to test whether ITD-1 blocks Activin A/Nodal and/or TGFβ signaling, which utilize the same intracellular signaling cascade through Smad4. ITD-1 strongly inhibits TGFβ2 signaling with similar efficacy (92% vs. 99% respectively), but with lower potency compared to SB-431542, an ACVR1B/TGFBR1 kinase inhibitor (IC50= 850nM vs. 70nM respectively), and is a weak and partial inhibitor of Activin A signals. ITD-1 selectively enhances the differentiation of uncommitted mesoderm to cardiomyocytes, but not to vascular smooth muscle and endothelial cells. ITD-1 reveals an unexpected role for TGFβ signaling in controlling cardiomyocyte differentiation from multipotent cardiovascular precursors.

分子结构图

ITD-1