MJ33

[Description]:

MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6[1]. MJ33 has a critical effect on inflammatory brain damage[2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase

Research Areas >> Inflammation/Immunology

[In Vitro]

MJ33, a transition-state analog competitive inhibitor of PLA2, inhibits the degradation of dipalmitoylphosphatidylcholine (DPPC) by ∼50% in both the whole lung and isolated alveolar type 2 cells. In vitro measurement of PLA2 activity in homogenate of lungs or isolated type 2 cells is markedly inhibited by MJ33 when assays at pH 4.0 in Ca2+-free medium but has no effect on Ca2+-dependent PLA2 activity at pH 8.5[3].

[In Vivo]

MJ33 (0.5 μM/kg ; by tail vein, at 24 h before MCAO) significantly blocks the increase IL-1β, IL-17 and IL-23 in rats stimulated by Prdx6 siRNA treatment[2]. Compared with the Prdx6 siRNA group, combined exposure to Prdx6 siRNA and MJ33 significantly downregulates the mRNA and protein expression of NF-κB, iNOS and COX-2[2]. Animal Model: Adult male Sprague-Dawley rats weighing 270-310 g (middle cerebral artery occlusion (MCAO) group) [2] Dosage: 0.5 μM/kg Administration: By tail vein, at 24 h before MCAO Result: Significantly blocked the increase IL-1β, IL-17 and IL-23 in rats stimulated by Prdx6 siRNA treatment.

[References]

[1]. Shanshan Y, et al. Phospholipase A2 of Peroxiredoxin 6 Plays a Critical Role in Cerebral Ischemia/Reperfusion Inflammatory Injury. Front Cell Neurosci. 2017 Apr 5;11:99.

[2]. Moawad AR, et al. Deficiency of peroxiredoxin 6 or inhibition of its phospholipase A2 activity impair the in vitro sperm fertilizing competence in mice. Sci Rep. 2017 Oct 11;7(1):12994.

[3]. Fisher AB, et al. Altered lung phospholipid metabolism in mice with targeted deletion of lysosomal-type phospholipase A2. J Lipid Res. 2005 Jun;46(6):1248-56.

[ Boiling Point ]:
522.7ºC at 760 mmHg

[ Molecular Formula ]:
C₂₂H₄₄F₃O₇P

[ Molecular Weight ]:
498.48300

[ Flash Point ]:
269.9ºC

[ Exact Mass ]:
498.29100

[ PSA ]:
86.86000

[ LogP ]:
7.63340

[ Vapour Pressure ]:
2.5E-12mmHg at 25°C

[ Storage condition ]:
2-8°C

Click to get detail MSDS

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Safety Phrases ]:
S22

[ RIDADR ]:
NONH for all modes of transport

1-Cys peroxiredoxin, a bifunctional enzyme with glutathione peroxidase and phospholipase A2 activities.

J. Biol. Chem. 275 , 28421, (2000)

This report provides definitive evidence that the protein 1-Cys peroxiredoxin is a bifunctional ("moonlighting") enzyme with two distinct active sites. We have previously shown that human, rat, and bo...

Fisher, A.B., Dodia, C.

Am. J. Physiol. Cell Physiol. 280 , 748, (2001)

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