RU-SKI 43 --- Hhat Inhibitor

Bioss

RU-SKI 43 --- Hhat Inhibitor [1043797-53-0]

16

Research Use Only

98.0

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 microM) . In vitro using purified Hhat and ShhN to analyze the kinetics of compounds inhibition of ShhN palmitoylation, RU-SKI 43 behaved as an uncompetitive inhibitor (Ki = 7.4 microM) with respect to Shh and as a noncompetitive inhibitor (Ki = 6.9 microM) 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

-20°C

51202000