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
CAS Number: 1043797-53-0
Molecular Weight: 386.55
Chemical Name: 2-((2-methylbutyl)amino)-1-(4-((m-tolyloxy)methyl)-3a, 4, 7, 7a-tetrahydrothieno[3, 2- c]pyridin-5(6H)-yl)ethanone
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
RU-SKI 43 was used at 10-20 µM final concentration in vitro and in cellular assays.
- Petrova E, et al. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling. (2013) Nat Chem Biol. 9(4):247-9.
- 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.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.