SB-239063 - p38 MAPK 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESB 239063Cat. No.: HY-11068CAS No.: 193551-21-2分式: CHFNO分量: 368.4作靶點(diǎn): p38 MAPK作通路: MAPK/ERK Pathway儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 33.33 mg/mL (90.47 mM; Need ultrasonic)H2O

2、 : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.79 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.79 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 SB 239063種有效、選擇性、可服的 p38 MAPK 抑制劑，對(duì)重 組純化的 p38 的 IC50 值為 44 nM，對(duì)

3、 p38 和 p38 的活性等效，但對(duì) p38 或 p38 所。具有抗哮喘作，還被于增強(qiáng)因衰或疾病受損的記憶，如阿爾茨海默病 1 2。IC50 & Target IC50: 44 nM (Human p38) 1體外研究 SB 239063 (0.110 M ; 29 hours, 47 hours) increases apoptosis of eosinophils in a dose-related in thepresence of 10 pM IL-5 at every time point from 21 hours onwards 1.SB 239063 potently inh

4、ibits IL-1 and TNF- a production in LPS-stimulated human peripheral bloodmonocytes with IC50 values of 120 nM and 350 nM, respectively 1.Apoptosis Analysis 1Cell Line: Eosinophils (guinea pig BALs)Concentration: 0.1M, 1M, 10MIncubation Time: 29 hours, 47 hoursResult: Increased apoptosis of eosinophi

5、ls in a dose-related in the presence of 10 pM IL-5 atevery time point from 21 hours onwards.體內(nèi)研究 SB 239063 (12 mg/kg; p.o.; 1 hour before and 4 hours after OA challenge; b.i.d. for 3 days) significantlyinhibits the resultant antigen-induced airway eosinophilia 1.SB 239063 (12 mg/kg; p.o.) almost abo

6、lishes ovalbumin (OA)-induced airway eosinophilia ( 93% inhibition)by inhalation 1.SB 239063 is a potent inhibitor of LPS-induced TNF-alpha production in the mouse peritoneal cavity with anEC50 of 5.8 mg/kg (2.810.3; 95% CL) 1.Animal Model: Male BALB/c mice (1820 g) 1Dosage: 12 mg/kgAdministration:

7、Oral administration; 1 h before and 4 h after OA challenge; bis in die for 3 daysResult: Significantly inhibited the resultant antigen-induced airway eosinophilia.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Carbohyd Polym. 2019 Mar 1;207:371-381. J Exp Clin Cancer Res. 2018 Jun 28;37(1):128. Int J Biol Macromol. 2018 Dec;120(Pt A)

8、:1039-1047. Front Pharmacol. 2017 Nov 14;8:808. Int Immunopharmacol. 2016 Sep;38:54-60.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Underwood DC, et al. SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophilinfiltration, and persistence. J Pharmacol Exp Ther. 2000 Apr;293(1):281-8.2. Matthew Huentelman, et al. Methods of treating memory loss and enhancing memory performance. US 20120245188 A1.McePdfHeightCaution: Product has not been fully validated for medical a