CAY10566 _SCD1 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECAY10566Cat. No.: HY-15823CAS No.: 944808-88-2分式: CHClFNO分量: 389.81作靶点: Stearoyl-CoA Desaturase (SCD)作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 8 mg/mL (2

2、0.52 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5654 mL 12.8268 mL 25.6535 mL5 mM 0.5131 mL 2.5654 mL 5.1307 mL10 mM 0.2565 mL 1.2827 mL 2.5654 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 CAY10566种硬脂酰辅酶 A 去饱和酶 1 (SCD1) 抑制剂。IC50 & Tar

3、get SCD1 1体外研究CAY10566 (0.0001-10 M; 24 hours) concentration-dependently decreases Swiss 3T3 cell proliferation 3.Cell Proliferation Assay 31/2 Master of Small Molecules 您边的抑制剂师www.MedChemECell Line: Swiss 3T3 cellsConcentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 MIncubation Time: 24 hoursResult: Swis

4、s 3T3 cell proliferation was concentration-dependently decreased.体内研究 After establishment of palpable tumors, the mice are treated with vehicle or SCD1 inhibitor (2.5 mg/kgCAY10566 orally twice daily). The effect of SCD1 inhibition on the Akt-driven tumors is greater than on theRas-driven tumors, wi

5、th the mean tumor volume at day 13 or 14 post therapy, relative to untreated tumors,0.50.04 and 0.670.05 respectively (P=0.01 for Ras-Akt comparison, by two-tailed t test) 2.REFERENCES1. Masuda M, et al. Activating transcription factor 4 regulates stearate-induced vascular calcification. J Lipid Res

6、. 2012 Aug;53(8):1543-52.2. Kamphorst JJ, et al. Hypoxic and Ras-transformed cells support growth by scavenging unsaturated fatty acids from lysophospholipids.Proc Natl Acad Sci U S A. 2013 May 28;110(22):8882-7.3. Koeberle A, et al. Palmitoleate is a mitogen, formed upon stimulation with growth factors, and converted to palmitoleoyl-phosphatidylinositol. J Biol Chem. 2012 Aug 3;287(32):27244-54.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Te