For research use only. Not Intended for Therapeutic Use!
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ITD-1 is an inducer of TGFβ type II receptor degradation-1, is a potent and highly selective TGFβ pathway inhibitor (IC50 = 0.85 μM).
IC50 value: 0.85 μM
in vitro: ITD-1 selectively enhances the differentiation of uncommitted mesoderm to cardiomyocytes, but not to vascular smooth muscle and endothelial cells. ITD-1 is the first selective TGFβ inhibitor and reveals an unexpected role for TGFβ signaling in controlling cardiomyocyte differentiation from multipotent cardiovascular precursors. ITD-1 downregulates HA-TGFBR2 and TGFBR2-mCherry with nearly the same potency (IC50 = 1.05 and 1.31 μM, respectively). ITD-1 acts by enhancing degradation rather than by blocking synthesis, which would affect cell surface and intracellular receptor pools equally.
. 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):242-252.