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.
For research use only. We do not sell to patients.
- CAS No.: 1043797-53-0
- Formula: C22H30N2O2S
- Molecular Weight:386.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) RU-SKI 43
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Biological Activity
Description
IC50 & Target
IC50: 850 nM (Hhat)[1]
Cellular Effect
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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 |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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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.
In Vivo
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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Molecular Weight 386.55
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Formula C22H30N2O2S
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SMILES
O=C(CNCC(C)CC)N1CCC2=C(C=CS2)C1COC3=CC=CC(C)=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[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
HY-18366 Related Classifications
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