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
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) RU-SKI 43
More
Biological Activity
IC50: 850 nM (Hhat)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | IC50 |
10 μM
Compound: 3, RU-SKI-43
|
Inhibition of SHh in mouse NIH3T3 cells assessed as Gli activation
Inhibition of SHh in mouse NIH3T3 cells assessed as Gli activation
|
10.1039/C3MD00334E |
| NIH3T3 | IC50 |
10 μM
Compound: 3, RU-SKI-43
|
Inhibition of SHh palmitoylation in mouse NIH3T3 cells
Inhibition of SHh palmitoylation in mouse NIH3T3 cells
|
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.
-
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).
-
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1043797-53-0
-
Molecular Weight 386.55
-
Formula C22H30N2O2S
-
SMILES
O=C(CNCC(C)CC)N1CCC2=C(C=CS2)C1COC3=CC=CC(C)=C3
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
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
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)
Powered by Bioz