RU-SKI 43 

RU-SKI 43 is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC₅₀ of 850 nM. RU-SKI 43 reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 has anti-cancer activity^[1].

IC50: 850 nM (Hhat)^[1]

RU-SKI 43 (10 μM; for 6 days) strongly decreases cell proliferation (83% in AsPC-1 cells) in AsPC-1 and Panc-1 cells^[2].
RU-SKI 43 (10 or 20 μM; 5 hours) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours^[1].
RU-SKI 43 (10 μM; for 72 hours) causes a 40% decrease in Gli-1 levels in AsPC-1 cells^[2].
RU-SKI 43 (10μM; 48 hours) results in decreased phosphorylation (47-67%) of four proteins in the Akt pathway, including Akt (phosphorylation at both Thr307 and Ser473), PRAS40, Bad and GSK-3β. RU-SKI 43 treatment also decreases phosphorylation of mTOR and S6, members of the mTOR signaling pathway^[2].
RU-SKI 43 behaves as an uncompetitive inhibitor (K_i=7.4 μM) with respect to Shh, and as a noncompetitive inhibitor (K_i=6.9 μM) with respect to ¹²⁵I-iodo-palmitoylCoA^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RU-SKI 43 has a t_1/2 of 17 min in mouse plasma after IV administration^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

386.55

C₂₂H₃₀N₂O₂S

1043797-53-0

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Petrova E, et al. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling.Nat Chem Biol. 2013 Apr;9(4):247-9.  [Content Brief]

  [2]. Petrova E, et al. Hedgehog acyltransferase as a target in pancreatic ductal adenocarcinoma. Oncogene. 2014 Jan 27. doi: 10.1038/onc.2013.575.  [Content Brief]