Biological Activity:? ITD-1 is a novel and highly selective TGFβ pathway inhibitor identified by a high throughput, embryonic stem cell (ESC) cardiac differentiation screening. ITD-1 promoted cardiomyocyte differentiation specifically via degradation of the TGFβ type II receptor (TGFBR2), effectively clearing the receptor from the cell surface and selectively inhibiting intracellular signaling (IC50?0.4–0.8 μM), revealing a role for TGFβ signaling mechanism as a repressor of cardiomyocyte fate. ITD-1 selectively enhanced the differentiation of uncommitted mesoderm to cardiomyocytes, but not to vascular smooth muscle and endothelial cells. In contrast to other commonly used TGFβ receptor (ALK) inhibitors, ITD-1 importantly only inhibits TGFβ signaling, but does not block the closely related Activin A signaling pathway, and represents a unique reagent for exploring TGFβ function in various biological contexts such as embryonic development and models of disease.
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How to Use:
In vitro:? ITD-1 was used at 5 μM final concentration in vitro and in cellular assays.
In vivo:?n/a
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Reference:
1. Willems E, et al. Small Molecule-Mediated TGF-β Type II Receptor Degradation Promotes Cardiomyogenesis in Embryonic Stem Cells. (2012) Cell Stem Cell.11(2):242-52.
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Products are for research use only. Not for human use.?