产品详情
简单介绍：
ITD-1,TGFβinhibitor
详情介绍：
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.
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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