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.
CAS Number: 1099644-42-4
Molecular Weight: 415.52
Chemical Name: ethyl 4-([1,1'-biphenyl]-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
ITD-1 was used at 5 µM final concentration in vitro and in cellular assays.
- 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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