| Bioactivity | ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM. | ||||||||||||||||||||||||||||||
| Target | IC50: 460 nM (TGFβ receptor)| Invitro |
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 | Name |
ITD-1 |
CAS |
1099644-42-4 |
Formula |
C27H29NO3 |
Molar Mass |
415.52 |
Appearance |
Solid |
Transport |
Room temperature in continental US; may vary elsewhere. |
Storage |
Reference |
[1]. Willems E, et al. Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells. Cell Stem Cell. 2012 Aug 3;11(2):242-52. |
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