ONX-0914-PR-957-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEONX-0914Cat. No.: HY-13207CAS No.: 960374-59-8Synonyms: PR-957分式: CHNO分量: 580.67作靶点: Proteasome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 : 35 mg/mL (60.28

2、mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.7221 mL 8.6107 mL 17.2215 mL5 mM 0.3444 mL 1.7221 mL 3.4443 mL10 mM 0.1722 mL 0.8611 mL 1.7221 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，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内

3、实验的作液，建议您现现配，当天使；澄清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: 2.17 mg/mL (3.74 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.17 mg/mL (3.74 mM); Clear solution1/2 Master of Small Molecules 您边的抑制

4、剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.17 mg/mL (3.74 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 ONX-0914 (PR-957)有效，选择性的免疫蛋酶体亚基LMP7的抑制剂。IC50 & Target IC50: 10 nM (LMP7) 1.体外研究 PR-957 blocked presentation of LMP7-specific, MHC-I-restricted antigens in vitro and in vivo. Select

5、iveinhibition of LMP7 by PR-957 blocked production of interleukin-23 (IL-23) by activated monocytes andinterferon-gamma and IL-2 by T cells 1.体内研究 In mouse models of rheumatoid arthritis and lupus, ONX-0914 treatment reverses signs of disease andresults in reductions in cellular infiltration, cytoki

6、ne production and autoantibody levels at well-tolerateddoses. The maximum tolerated dose (MTD) of ONX-0914 in mice to be 30 mg/kg body weight. IFN-g releaseis inhibited by 60% at LMP7-selective concentrations of ONX-0914 and by 90% at higher concentrations.Production of IL-2 is also inhibited by 50%

7、 1.PROTOCOLCell Assay Stock solutions of PR-957 was prepared in DMSO and were diluted 400-fold for cell treatments. Drugtreatments were performed in RPMI-1640 media containing 5% FBS, 100 units/ml penicillin and 100 g/mlstreptomycin. Cells were exposed to PR-957 or 0.25% DMSO at 37C for a 1 hr perio

8、d followed by fourwashes with media (RPMI-1640 containing 5% FBS) prior to either stimulation or washing twice with mediaand twice with phosphate buffered saline (PBS), lysis in hypotonic TE buffer (20 mM Tris HCL and 5 mMEDTA pH 8.0), and storage at -80C for the active site ELISA. Tissue culture me

9、dia and fetal bovine serum(FBS) were purchased from Mediatech or Invitrogen-Life Technologies.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Biochem Pharmacol. 2018 Oct;156:511-523.See more customer validations on HYPERLINK / www.MedChemERE

10、FERENCES1. Muchamuel T, et al. A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progressionof experimental arthritis. Nat Med. 2009 Jul;15(7):781-7.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product has not been fully valida