生物活性 PNRI-299 is a selective AP-1 transcription inhibitor with an IC50 of 20 uM. PNRI-299 is a selective APE/Ref-1 inhibitor. PNRI-299 has no effect on NF-κB transcription or thioredoxin (up to 200 uM). PNRI-299 significantly reduces airway eosinophil infiltration, mucus hypersecretion, edema, and IL-4 levels in a mouse asthma model[1][2][3].
体外研究(In Vitro) PNRI-299 specifically reacts with Ref-1, inhibits AP-1 transcription, and overexpression of the molecular target. Ref-1 attenuates PNRI-299 inhibition of AP-1 transcription. PNRI-299 interacts with the redox nucleophile Cys-65, to aid in the interpretation of structure activity relationships (SARs)[1].
体内研究(In Vivo) PNRI-299 (intranasal; 0.75 or 2.0 mg/kg; 30 min before OVA on days 25-27) reduces the airway inflammatory cell infiltration (arrows) and mucus release in ovalbumin (OVA)-treated (i.p.; 100 μg) female BALB/c mice aged 6-8 wk)[1]. PNRI-299 (3, 10 mg/kg; iv; 5 min before reperfusion) has no significant effect on the translocation of NF-κB in male C57/BL6 mice (8-10 weeks). PNRI-299 has little effect on the inflammatory response that follows intestinal I/R injury[2].
分子量 401.37
Formula C21H15N5O4
CAS 号 550368-41-7
运输条件 Room temperature in continental US; may vary elsewhere.
储存方式 Please store the product under the recommended conditions in the Certificate of Analysis.