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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 | Availability | 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] |
Alias | 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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