ML349 - Phospholipase 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEML349Cat. No.: HY-100737CAS No.: 890819-86-0分式: CHNOS分量: 454.56作靶点: Phospholipase作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 20 mg/mL (44.00 mM; Need ultrasonic)Mass

2、 Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1999 mL 10.9996 mL 21.9993 mL5 mM 0.4400 mL 2.1999 mL 4.3999 mL10 mM 0.2200 mL 1.1000 mL 2.1999 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。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指

3、该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2 mg/mL (4.40 mM); Suspended solution; Need ultrasonicBIOLOGICAL ACTIVITY物活性 ML349个有效且特异的酰 蛋硫酯酶 2 (APT-2) 抑制剂，其 Ki 值为 120 nM。ML349 也LYPLA2 的抑制剂，其 IC50 值为 144 nM。1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEIC50

4、& Target Ki: 120 nM (APT-2) 1IC50: 144 nM (LYPLA2) 2体外研究 ML349 is an inhibitor of acyl protein thioesterase 1 and 2 (APT-1 and APT-2) with Kis of 10000 and 12020nM, respectively 1. ML349 is also an inhibitor of both LYPLA1 and LYPLA2 with IC50s of 3000 and 144nM, respectivley 2. ML348 and ML349 do n

5、ot decrease cell viability, but they lead to a slight activation ofAKT in NRAS mutant cells 3.PROTOCOLCell Assay 3 Cells are plated in 96-well plates with a density of 4000 to 8000 cells per well and incubated for 24 h at 37Cwith 5% CO2. Then cells are treated with increasing drug (including ML349)

6、concentrations and theircombinations. Cell viability is measured with the cell viability assay according to the manufacturers protocol3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Won SJ, et al. Molecular Mechanism for Isoform-Selective

7、 Inhibition of Acyl Protein Thioesterases 1 and 2 (APT1 and APT2). ACSChem Biol. 2016 Dec 16;11(12):3374-3382.2. Adibekian A, et al. Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 2 (LYPLA2).3. Vujic I, et al. Acyl protein thioesterase 1 and 2 (APT-1, APT-2) inhibitors palmostatin B, ML348 and ML349 have different effects onNRAS mutant melanoma cells. Oncotarget. 2016 Feb 9;7(6):7297-306.McePdfHeightCaution: Product has not been fully validated for medical applications.For rese