AKR1C3-IN-1-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAKR1C3-IN-1Cat. No.: HY-107379CAS No.: 327092-81-9分式: CHNOS分量: 317.36作靶点: Others作通路: Others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 : 100 mg/mL (315.10 mM)* means soluble, but saturati

2、on unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1510 mL 15.7550 mL 31.5100 mL5 mM 0.6302 mL 3.1510 mL 6.3020 mL10 mM 0.3151 mL 1.5755 mL 3.1510 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 AKR1C3-IN-1种有效的，度选择性的 AKR1C3 抑制剂，IC50 值为 13 nM。IC50 & Target IC50: 13 n

3、M (AKR1C3) 1体外研究AKR1C3-IN-1 shows less potent activities with 20.33.8 M against AKR1C1 and 30 M against AKR1C2and AKR1C4. AKR1C3-IN-1 inhibits AKR1C3 activity (inhibiting PR-104H formation) with an IC50 of1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE0.0270.002 M 1.PROTOCOLKinase Assay 1 A compet

4、itive fluorescence assay is used to measure AKR1C enzyme activity, where a nonfluorescentketone probe (probe 5) selective for the AKR1C enzyme isoforms is reduced to a fluorescent alcohol in thepresence of AKR1C enzyme and NADPH. Briefly, purified protein (2 g/mL AKR1C1, 1 g/mL AKR1C2, 2 g/mL AKR1C3

5、, and 5 g/mL AKR1C4) are incubated with 40 M probe 5, AKR1C3-IN-1, and 50 M NADPHin an assay buffer of 10 mM MOPS (pH=7.2), 130 mM NaCl, 1 mM DTT, and 0.01% Triton-X-100 for 1 h at37C. The reaction is stopped by addition of 35 mM NaOH, and fluorescence is read in a SpectraMax M2microplate reader at

6、excitation/emission wavelengths of 420/510 nM. The compounds and known AKR1C3inhibitors (flufenamic acid, indomethacin, naproxen, meclofenamic acid, S(+)-ibuprofen and flurbiprofen) aretested at multiple concentrations between 0.1 nM and 100 M in 2% DMSO to generate AKR1C enzymeinhibition data. Comp

7、ound IC50 values are calculated by fitting the inhibition data to a four-parameter logisticsigmoidal dose-response curve using Prism 5.02.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Jamieson SM, et al. 3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-hydroxysteroid dehydrogenase AKR1C3. J Med Chem. 2012 Sep 13;55(17):7746-58.McePdfHeightCaution: Product has not been fully validated for medical applications.For re