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:
Reference:
Products are for research use only. Not for human use.
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