For research use only. Not for therapeutic Use.
Hh-Ag1.5 (SAg1.5) is a potent Hedgehog (Hh) agonist with an EC50 of 1 nM[1]. Hh-Ag1.5 mediated reprogramming breaks the quiescence of noninjured liver stem cells for rescuing liver failure[2].
HhAg1.5 (5 μM; for 3 weeks) facilitates dramatic expansion of quiescent CD133+ CD45- liver stem cells (Hh3A cells) enriched from non-injured liver in vitro[2].
Hh-Ag1.5 competely binds to the Smo-containing membranes with the Ki value of 0.52 nM[3].
The Smo agonist SAG-1.5 displays nanomolar-range potency stimulation of Gli-responsive reporter activity, with an EC50 of 7 nM[4].
| Catalog Number | R030630 |
| CAS Number | 612542-14-0 |
| Synonyms | 3-chloro-4,7-difluoro-N-[4-(methylamino)cyclohexyl]-N-[(3-pyridin-4-ylphenyl)methyl]-1-benzothiophene-2-carboxamide |
| Molecular Formula | C28H26ClF2N3OS |
| Purity | ≥95% |
| InChI | InChI=1S/C28H26ClF2N3OS/c1-32-20-5-7-21(8-6-20)34(16-17-3-2-4-19(15-17)18-11-13-33-14-12-18)28(35)27-25(29)24-22(30)9-10-23(31)26(24)36-27/h2-4,9-15,20-21,32H,5-8,16H2,1H3 |
| InChIKey | RXZDWPYJFCAZCW-UHFFFAOYSA-N |
| SMILES | CNC1CCC(CC1)N(CC2=CC(=CC=C2)C3=CC=NC=C3)C(=O)C4=C(C5=C(C=CC(=C5S4)F)F)Cl |
| Reference | [1]. Randall W King. Roughing Up Smoothened: Chemical Modulators of Hedgehog Signaling. J Biol. 2002 Nov 6;1(2):8. [2]. Abhisek Mitra, et al. A Small Molecule Hedgehog Agonist HhAg1.5 Mediated Reprogramming Breaks the Quiescence of Noninjured Liver Stem Cells for Rescuing Liver Failure. Transl Res. 2019 Mar;205:44-50. [3]. Maria Frank-Kamenetsky, et al. Small-molecule Modulators of Hedgehog Signaling: Identification and Characterization of Smoothened Agonists and Antagonists. J Biol. 2002 Nov 6;1(2):10. [4]. Cynthia M Rominger, et al. Evidence for Allosteric Interactions of Antagonist Binding to the Smoothened Receptor. J Pharmacol Exp Ther. 2009 Jun;329(3):995-1005. |
