RU-SKI 43 hydrochloride - ≥99% , CAS No.1782573-67-4

CAS: 1782573-67-4 Cat. No.: R648984 Peso molecular: 423.01

GRADE & PURITY ≥99%

Storage

Store at 2-8°C,Desiccated

Shipped In

Wet ice

Descripción general

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.

Form:Solid

IC50& Target:IC50: 850 nM (Hhat)

Specifications

Especificaciones y pureza

≥99%

Mecanismos bioquímicos y fisiológicos

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

Condiciones de almacenamiento de almacenamiento

Store at 2-8°C, Desiccated

Enviado en

Wet ice

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Pureza

≥99%

Nombres e identificadores

• Sonrisas canónicas: [H]Cl.O=C(CNCC(C)CC)N1CCC2=C(C=CS2)C1COC3=CC=CC(C)=C3
• Peso molecular: 423.01

Propiedades químicas y físicas

• Solubilidad: DMSO : ≥ 51 mg/mL (120.56 mM) H2O : 2.5 mg/mL (5.91 mM; Need ultrasonic)