RU-SKI 43
Based on 2 publication(s) in Google Scholar
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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- CAS No.: 1043797-53-0
- Formule: C22H30N2O2S
- Masse moléculaire:386.55
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) RU-SKI 43
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Activité biologique
IC50: 850 nM (Hhat)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | IC50 |
10 μM
Compound: 3, RU-SKI-43
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Inhibition of SHh in mouse NIH3T3 cells assessed as Gli activation
Inhibition of SHh in mouse NIH3T3 cells assessed as Gli activation
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10.1039/C3MD00334E |
| NIH3T3 | IC50 |
10 μM
Compound: 3, RU-SKI-43
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Inhibition of SHh palmitoylation in mouse NIH3T3 cells
Inhibition of SHh palmitoylation in mouse NIH3T3 cells
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10.1039/C3MD00334E |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AsPC-1 and Panc-1 pancreatic cancer cells
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Concentration:10 μM
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Incubation Time:For 6 days (drugs were replenished every 48 hours)
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Result:Strongly decreased cell proliferation (83% in AsPC-1 cells).
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Cell Line:COS-1 cells expressing HA-Hhat and Shh
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Concentration:10 or 20 μM
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Incubation Time:5 hours
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Result:Caused dose-dependent inhibition of Shh palmitoylation following only 5 hours.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1043797-53-0
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Masse moléculaire 386.55
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Formule C22H30N2O2S
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SMILES
O=C(CNCC(C)CC)N1CCC2=C(C=CS2)C1COC3=CC=CC(C)=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Exp Cell Res
2024 Jun 1;439(1):114072. PMID: 38719175 -
Dent J (Basel)
Effects of Improper Mechanical Force on the Production of Sonic Hedgehog, RANKL, and IL-6 in Human Periodontal Ligament Cells In Vitro. [Abstract]2024 Apr 15;12(4):108. PMID: 38668020
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RU-SKI 43 Related Classifications
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