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RU-SKI 43

Catalog No. T12797 CAS 1043797-53-0

Synonyms: RUSKI 43

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

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RU-SKI 43, CAS 1043797-53-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
5 mg	In stock	$ 110.00
10 mg	In stock	$ 157.00
25 mg	In stock	$ 375.00
50 mg	In stock	$ 557.00
1 mL * 10 mM (in DMSO)	In stock	$ 118.00

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Purity: 99.78%

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Description	RU-SKI 43 is a potent and selective hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM.RU-SKI 43 has anticancer activity and is a potential compound for the treatment of lung adenocarcinomas.RU-SKI 43 reduces Gli-1 activation through smoothing-independent non-canonical signalling 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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Petrova E, et al. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling.Nat Chem Biol. 2013 Apr;9(4):247-9. 2. Petrova E, et al. Hedgehog acyltransferase as a target in pancreatic ductal adenocarcinoma. Oncogene. 2014 Jan 27.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Membrane Protein-targeted Compound Library Inhibitor Library GPCR Compound Library Anti-Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

RU-SKI 43 1043797-53-0 GPCR/G Protein Metabolism Stem Cells Hedgehog/Smoothened Acyltransferase RUSKI-43 RUSKI43 RUSKI 43 inhibitor inhibit

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