Sulfasalazine-NSC-667219-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESulfasalazineCat. No.: HY-14655CAS No.: 599-79-1Synonyms: NSC 667219分式: CHNOS分量: 398.39作靶点: NF-B; Autophagy作通路: NF-B; Autophagy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 : 80 mg/mL (200.

2、81 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5101 mL 12.5505 mL 25.1010 mL5 mM 0.5020 mL 2.5101 mL 5.0202 mL10 mM 0.2510 mL 1.2551 mL 2.5101 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，体内实验的作液，

3、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: 2.5 mg/mL (6.28 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.28 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.Me

4、dChemEBIOLOGICAL ACTIVITY物活性 Sulfasalazine治疗类风湿关节炎和溃疡性结肠炎的药物。报道显Sulfasalazine可抑制 NF-B 的活性。IC50 & Target RelA Autophagy体外研究 Treatment of SW620 colon cells with sulfasalazine inhibits TNF-, LPS-, or phorbol ester-induced NFBactivation. NFBdependent transcription is inhibited by sulfasalazine at micro-

5、 to millimolar concentrations.TNF-induced nuclear translocation of NFB is prevented by sulfasalazine through inhibition of IBdegradation 1. Preincubation with 5 m M of sulfasalazine alone significantly increases basal m RNA expression ofall proinflam m atory cytokines with levels of IL6 m RNA increa

6、sed by 80fold com pared with vehicle control 2. Oncedigested, sulfasalazine is cleaved into sulfapyridine and 5-am inosalicylic acid by colonic bacteria, and the latter, too, isreported to suppress NF-kappaB activity 3.体内研究 At low doses (0.25 mM), SAS is able to suppress glioma growth by over 60% co

7、mpared to untreated controls3.PROTOCOLKinase Assay NF-B MCE has not independently confirmed the accuracy of these methods. They are for reference only.1Cell Assay 1 Sulfasalazine is dissolved in culture medium. SW620 cells are grown in Dulbeccos modified Eagle medium,supplemented with 10% heat-inact

8、ivated FCS, 2 mmol/liter glutamine, and 1% (wt/vol)penicillin/streptomycin. SW620 cells are transfected with the 3xIgkBLuc reporter construct. After 18 h, cellsare incubated with either medium alone or with sulfasalazine (0.1, 0.2, 0.5, 1, 2, 5 mM) before stimulationwith TNF, LPS, or PMA. Luciferase

9、 assay is performed 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Sulfasalazine is dissolved in 0.1 M NaOH, and then neutralized by titrating with 0.1 M HCl. U-87MGAdministration 3 glioma cells are implanted into the cranium of a SCID m

10、ouse. After 7 days, animals are randomized intothree groups of five animals each. One group receives 1 mL i.p. saline injections twice daily for 3 weeks. Thetwo test groups receives 8 mg of sulfasalazine in 1 mL saline twice daily for 3 weeks. Tumor growth andanimal health were monitored. After perf

11、usion with 4% paraformaldehyde, mouse brains were collected,rinsed, and placed in 30% sucrose 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Wahl C, et al. Sulfasalazine: a potent and specific inhibitor of nuclear factor kappa B. J Clin

12、Invest. 1998 Mar 1;101(5):1163-74.2. Sykes L, et al. Sulfasalazine augments a pro-inflammatory response in interleukin-1-stimulated amniocytes and myocytes.Immunology. 2015 Dec;146(4):630-44.3. Chung WJ, et al. Sulfasalazine inhibits the growth of primary brain tumors independent of nuclear factor-kappaB. J Neurochem. 2009Jul;110(1):182-93.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMcePdfHeightCauti