WZ4003 - AMPK 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEWZ4003Cat. No.: HY-15802CAS No.: 1214265-58-3分式: CHClNO分量: 496.99作靶点: AMPK作通路: Epigenetics; PI3K/Akt/mTOR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 : 24.5 mg/mL (49.30 mM; Need ultrasoni

2、c and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0121 mL 10.0606 mL 20.1211 mL5 mM 0.4024 mL 2.0121 mL 4.0242 mL10 mM 0.2012 mL 1.0061 mL 2.0121 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 WZ4003种有效的，度特异性的 NUAK kinase 抑制剂，能够抑制 NUAK1 (ARK5)/NUAK2 的活性，IC50值分别

3、为 20 nM/100 nM。IC50 & Target NUAK1 NUAK220 nM (IC50) 100 nM (IC50)体外研究WZ4003 (3-10 M) markedly suppresses NUAK1-mediated MYPT1 phosphorylation, in HEK-293 cells1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEexpressing wild-type NUAK1. Moreover, WZ4003 (10 M) inhibits MYPT1 Ser445 phosphorylation a

4、s well ascell migration, invasion and proliferation to a similar extent as knock out in MEFs or knock down in U2OScells of NUAK1 1. WZ4003 also exhibits a high, specific affinity to the L858R/T790M mutant EGFR, while asignificantly reduced cellular IC50 against T790M containing Ba/F3 cells 2.PROTOCO

5、LKinase Assay 1 In vitro activities of purified GST-NUAK1 and GST-NUAK1A195T are measured using Cerenkov counting ofincorporation of radioactive 32P from -32PATP into Sakamototide substrate peptide. Reactions are carriedout in a 50 L reaction volume for 30 min at 30C and reactions are terminated by

6、spotting 40 L of thereaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples arewashed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. Thekinase-mediated incorporation of -32PATP into Sakamototide is quantified by Cere

7、nkov counting. One unitof activity is defined as that which catalysed the incorporation of 1 nmol of 32Pphosphate into the substrateover 1 h.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 Cell proliferation assays are carried out colorimet

8、rically in 96-well plates. Initially, 2000 cells per well areseeded for U2OS cells and 3000 cells per well are seeded for MEFs. The proliferation assays are carried outover 5 days in the presence or absence of 10 M HTH-01-015 or WZ4003.MCE has not independently confirmed the accuracy of these method

9、s. They are for reference only.户使本产品发表的科研献 Cancer Discov. 2018 May;8(5):632-647. J Cell Biol. 2019 Apr 1;218(4):1369-1389. Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Banerjee S, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAKkinases. Biochem J. 2014 Jan 1;457(1):215-25.2. Zhou W, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4McePdfHeightCaution: Product has not been fully validate