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RU-SKI 43 is a potent and selective hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. It exhibits anticancer activity and is a potential treatment for lung adenocarcinomas. RU-SKI 43 reduces Gli-1 activation through smoothening-independent non-canonical signaling and inhibits Akt and mTOR pathway activity.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $45 | - | In Stock | |
| 5 mg | $110 | - | In Stock | |
| 10 mg | $157 | - | In Stock | |
| 25 mg | $375 | - | In Stock | |
| 50 mg | $557 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $118 | - | In Stock |
| Description | RU-SKI 43 is a potent and selective hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. It exhibits anticancer activity and is a potential treatment for lung adenocarcinomas. RU-SKI 43 reduces Gli-1 activation through smoothening-independent non-canonical signaling and inhibits Akt and mTOR pathway activity. |
| Targets&IC50 | Hhat:850 nM, [125I]-iodo-palmitoylCoA:6.9 μM(Ki), Shh:7.4 μM(Ki) |
| In vitro | RU-SKI 43 (10 or 20 μM; 5 h; AsPC-1 and Panc-1 pancreatic cancer cells) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours.[1] RU-SKI 43 acts as an uncompetitive inhibitor with a Ki of 7.4 μM concerning Shh, while it functions with a Ki of 6.9 μM regarding 125I-iodo-palmitoylCoA.[1] RU-SKI 43 (10μM; 48 h; AsPC-1 and Panc-1 pancreatic cancer cells) leads to reduced phosphorylation (47-67% decrease) of four proteins within the Akt pathway, which encompass Akt (phosphorylated at Thr307 and Ser473), PRAS40, Bad, and GSK-3β. Additionally, RU-SKI 43 treatment results in decreased phosphorylation of mTOR and S6, both of which are constituents of the mTOR signaling pathway.[2] 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 μM; for 72 h; AsPC-1 and Panc-1 pancreatic cancer cells) causes a 40% decrease in Gli-1 levels in AsPC-1 cells.[2] |
| In vivo | After IV administration,RU-SKI 43 has a t1/2 of 17 min in mouse plasma.[1] |
| Synonyms | RUSKI 43 |
| Molecular Weight | 386.55 |
| Formula | C22H30N2O2S |
| Cas No. | 1043797-53-0 |
| Smiles | C(OC1=CC(C)=CC=C1)C2C3=C(CCN2C(CNCC(CC)C)=O)SC=C3 |
| Relative Density. | 1.31g/cm3 |
| Storage | store at low temperature | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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