| Molecular Weight: | 388.57 |
| Formula: | C22H32N2O2S |
| Purity: | ≥ 98% |
| CAS#: | 1043797-53-0 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | 2-((2-methylbutyl)amino)-1-(4-((m-tolyloxy)methyl)-3a,4,7,7a-tetrahydrothieno[3,2-c]pyridin-5(6H)-yl)ethanone |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
RU-SKI 43 is the first potent and specific small molecule inhibitor of Hedgehog acyltransferase (Hhat), and directly inhibits palmitoylation of the Shh ligand. It was discovered by a high-throughput screen using a peptide-based assay to monitor Hhat-mediated Shh palmitoylation (IC50 ~0.85 µM). In vitro using purified Hhat and ShhN to analyze the kinetics of compound’s inhibition of ShhN palmitoylation, RU-SKI 43 behaved as an uncompetitive inhibitor (Ki = 7.4 μM) with respect to Shh and as a noncompetitive inhibitor (Ki = 6.9 μM) with respect to [125I]iodo-palmitoyl CoA. In cells, RU-SKI 43 specifically blocks Shh palmitoylation and inhibits autocrine and paracrine Shh signaling. Hhat inhibitor could offer a new treatment modality for cancers characterized by Shh overexpression and extremely poor prognoses.
How to Use:
- In vitro: RU-SKI 43 was used at 10-20 µM final concentration in vitro and in cellular assays.
- In vivo: n/a
Reference:
- 1. Petrova E, et al. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling. (2013) Nat Chem Biol. 9(4):247-9.
- 2. Petrova E, et al. Hedgehog acyltransferase as a target in pancreatic ductal adenocarcinoma. (2014) Oncogene. In press.
Products are for research use only. Not for human use.
