For research use only. Not for therapeutic Use.
More active (+)-enantiomer of ITD 1 (Axon 2323), a selective inhibitor of TGFβ/Smad signaling (IC50 values 0.46 μM and 6.90 μM for (+)-ITD 1 and (−)-ITD 1, respectively for TGF-β inhibition) that acts by clearing the type II TGFβ receptor from the cell surface. ITD 1 stimulates the differentiation of cardiomyocytes and promote cardiogenesis in murine embryonic stem cell (mESCs). TGFβ inhibition by the (+)-enantiomer is approximately 15-fold more effective than by its (−)-enantiomer.
KEYWORDS: (+)-ITD-1 | supplier | TGF-βR2 inhibitor | ITD1 | (+)-ITD1 | CAS [1409968-46-2] | [1099644-42-4] | [1217467-13-4] | TGF-β | TGF-βR | Antagonist | active enantiomer | Smad | differentiation | cardiomyocytes | cardiogenesis | mESC | stem cell
| Catalog Number | I047612 |
| CAS Number | 1409968-46-2 |
| Molecular Formula | C27H29NO3 |
| Purity | ≥95% |
| IUPAC Name | ethyl 2,7,7-trimethyl-5-oxo-4-(4-phenylphenyl)-1,4,6,8-tetrahydroquinoline-3-carboxylate |
| 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 |
| SMILES | CCOC(=O)C1=C(NC2=C(C1C3=CC=C(C=C3)C4=CC=CC=C4)C(=O)CC(C2)(C)C)C |
| Reference | D. Schade et al. Synthesis and SAR of b-annulated 1,4-dihydropyridines define cardiomyogenic compounds as novel inhibitors of TGFβ signaling. J. Med. Chem. 2012, 55, 9946-9957.
E. Willems et al. Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells. Cell Stem Cell. 2012, 11, 242-252. |
