ITD-1, TGFβ inhibitor


Catalog No. size PriceQuantity
M60060-2D 10 mM in DMSO (0.482 mL) $139
M60060-2S 2mg solid $139
M60060-10S 10mg solid $549

Description

Product Information
Molecular Weight: 415.52
Formula: C27H29NO3
Purity: ≥98%
CAS#: 1099644-42-4
Solubility: DMSO up to 50 mM
Chemical Name: ethyl 4-([1,1'-biphenyl]-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

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.

 

How to Use:

 

  • In vitro:  ITD-1 was used at 5 µM final concentration in vitro and in cellular assays.
  • In vivo: n/a

 

 

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.
 
 

Products are for research use only. Not for human use. 

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