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RU-SKI 43

Catalog No. T12797Cas No. 1043797-53-0
Alias RUSKI 43

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.

RU-SKI 43

RU-SKI 43

Purity: 99.78%
Catalog No. T12797Alias RUSKI 43Cas No. 1043797-53-0
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 SizePriceAvailabilityQuantity
1 mg$45In Stock
5 mg$110In Stock
10 mg$157In Stock
25 mg$375In Stock
50 mg$557In Stock
1 mL x 10 mM (in DMSO)$118In Stock
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Purity:99.78%
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Product Introduction

Bioactivity
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
Shh:7.4 μM(Ki), Hhat:850 nM, [125I]-iodo-palmitoylCoA:6.9 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]
AliasRUSKI 43
Chemical Properties
Molecular Weight386.55
FormulaC22H30N2O2S
Cas No.1043797-53-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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