ITD-1

• CAT Number: I000412
• CAS Number: 1099644-42-4
• Molecular Formula: C₂₇H₂₉NO₃
• Molecular Weight: 415.52
• Purity: ≥95%
• Target: TGF-β Receptor
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 0.85 μM
• InChI: InChI=1S/C27H29NO3/c1-5-31-26(30)23-17(2)28-21-15-27(3,4)16-22(29)25(21)24(23)20-13-11-19(12-14-20)18-9-7-6-8-10-18/h6-14,24,28H,5,15-16H2,1-4H3
• InChIKey: ULFUJLFTRWWLPO-UHFFFAOYSA-N
• SMILES: O=C(C1=C(C)NC2=C(C(CC(C)(C)C2)=O)C1C3=CC=C(C4=CC=CC=C4)C=C3)OCC

ITD-1(CAT: I000412) acts as an inducer of TGFβ type II receptor degradation-1, presenting as a potent and highly selective inhibitor of the TGFβ pathway. In vitro, ITD-1 showcases its selectivity by promoting the differentiation of uncommitted mesoderm into cardiomyocytes, demonstrating no influence on vascular smooth muscle or endothelial cells. As the first selective TGFβ inhibitor, ITD-1 unveils an unanticipated role for TGFβ signaling in orchestrating cardiomyocyte differentiation from multipotent cardiovascular precursors. It achieves its effects by enhancing the degradation of HA-TGFBR2 and TGFBR2-mCherry receptors, highlighting its mechanistic focus on enhancing degradation over blocking synthesis.

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):242-252.