| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| R655658-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $145.90 |
| Specifications & Purity | 10mM in DMSO |
|---|---|
| Storage Temp | Desiccated,Store at -80°C |
| Shipped In | Ice chest + Ice pads |
| Product Description | RU-SKI 43 hydrochloride is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC 50 of 850 nM. RU-SKI 43 hydrochloride reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 hydrochloride has anti-cancer activity In Vitro RU-SKI 43 hydrochloride (10 μM; for 6 days) strongly decreases cell proliferation (83% in AsPC-1 cells) in AsPC-1 and Panc-1 cells. RU-SKI 43 hydrochloride (10 or 20 μM; 5 hours) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours. RU-SKI 43 hydrochloride (10 μM; for 72 hours) causes a 40% decrease in Gli-1 levels in AsPC-1 cells. RU-SKI 43 hydrochloride (10 μM; 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. RU-SKI 43 hydrochloride 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 125 I-iodo-palmitoylCoA. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell 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 AnalysisCell 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 hydrochloride has a t 1/2 of 17 min in mouse plasma after IV administration . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:IC50: 850 nM (Hhat) |
| Canonical SMILES | [H]Cl.O=C(CNCC(C)CC)N1CCC2=C(C=CS2)C1COC3=CC=CC(C)=C3 |
|---|---|
| Molecular Weight | 423.01 |
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