Porcn-IN-1 - Porcupine 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPorcn-IN-1Cat. No.: HY-111472CAS No.: 2036044-77-4分式: CHFNO分量: 410.44作靶點(diǎn): Porcupine作通路: Stem Cell/Wnt儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (243.64 mM)* means soluble, bu

2、t saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.4364 mL 12.1820 mL 24.3641 mL5 mM 0.4873 mL 2.4364 mL 4.8728 mL10 mM 0.2436 mL 1.2182 mL 2.4364 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Porcn-IN-1是有效的 porcupine 抑制劑，IC50 值為 0.50.2 nM。IC50 & Target

3、IC50: 0.50.2 nM (Porcupine inhibitor) 1體外研究Porcupine is an enzyme that catalyses the addition of palmitoleate to a serine residue in Wnt proteins, aprocess which is required for the secretion of Wnt proteins. Porcupine-IN-1 is as potent as the clinical1/2 Master of Small Molecules 您邊的抑制劑師www.MedChem

4、Ecompound LGK974 in a cell based STF reporter gene assay. Porcn-IN-1 potently inhibits the secretion ofWnt3A, therefore is confirmed to be a porcupine inhibitor 1.體內(nèi)研究 Porcn-IN-1 demonstrates moderate clearance under the treatment of human liver microsomes (57mL/min/kg) and rat liver microsomes (24

5、mL/min/kg). It exhibits high clearance when treated with mousemicrosomes (109 mL/min/kg) 1.PROTOCOLCell Assay 1 HEK293T cells are transfected with pLinbin-Wnt3A plasmid or vehicle control. The HEK293T cells are thentreated with or without compounds (Porcn-IN-1). Western Blot is used after 48 h to an

6、alyze both the cell lysisand culture medium 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Xu Z, et al. Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the reversed amidescaffold.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 40