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ITD-1

ITD-1 是第一个选择性的 TGFβ 受体抑制剂,IC50 为 460 nM。

  • 货号:
    TK0483
  • 规格:
    1mg
    5mg
    10mg
    50mg
  • 价格:
    0.00

产品参数

CAS No.1099644-42-4
生物活性ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM.
分子式C27H29NO3
分子量415.52
运输条件Room temperature in continental US; may vary elsewhere.
储存条件 Powder -20°C 3 years
溶解性数据DMSO : 28 mg/mL (67.39 mM; Need ultrasonic and warming)
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.
文献•ACS Comb Sci. 2019 Dec 9;21(12):805-816. •Oncotarget. 2017 Dec 14;9(3):3188-3197.
纯度及产品资料98%