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  3. RU-SKI 43

RU-SKI 43 

Cat. No.: HY-18366
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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.

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RU-SKI 43 Chemical Structure

RU-SKI 43 Chemical Structure

CAS No. : 1043797-53-0

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Description

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 & Target

IC50: 850 nM (Hhat)[1]

In Vitro

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 (Ki=7.4 μM) with respect to Shh, and as a noncompetitive inhibitor (Ki=6.9 μM) with respect to 125I-iodo-palmitoylCoA[1].

Cell Proliferation Assay[2]

Cell Line: AsPC-1 and Panc-1 pancreatic cancer cells
Concentration: 10 μM
Incubation Time: For 6 days (drugs were replenished every 48 hours)
Result: Strongly decreased cell proliferation (83% in AsPC-1 cells).

Western Blot Analysis[1]

Cell Line: COS-1 cells expressing HA-Hhat and Shh
Concentration: 10 or 20 μM
Incubation Time: 5 hours
Result: Caused dose-dependent inhibition of Shh palmitoylation following only 5 hours.
In Vivo

RU-SKI 43 has a t1/2 of 17 min in mouse plasma after IV administration[1].

Molecular Weight

386.55

Formula

C₂₂H₃₀N₂O₂S

CAS No.

1043797-53-0

SMILES

O=C(CNCC(C)CC)N1CCC2=C(C=CS2)C1COC3=CC=CC(C)=C3

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

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Keywords:

RU-SKI 43HedgehogacyltransferaseHhatGli-1Smoothened-independentnon-canonicalAktmTORanti-cancerInhibitorinhibitorinhibit

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