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MF63

Cat. No. M1737
MF63 Structure
Size Price Availability Quantity
5mg USD 60 In stock
10mg USD 90 In stock
50mg USD 200 In stock
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Quality Control
Biological Activity

MF63 potently inhibited the human mPGES-1 enzyme (IC50=1.3 nM), with a high degree (>1000-fold) of selectivity over other prostanoid synthases. Microsomal prostaglandin E synthase-1 (mPGES-1) is a terminal prostaglandin E (2) (PGE (2)) synthase in the cyclooxygenase pathway. Inhibitors of mPGES-1 may block PGE (2) production and relieve inflammatory symptoms. In rodent species, MF63 strongly inhibited guinea pig mPGES-1 (IC50=0.9 nM) but not the mouse or rat enzyme. In addition, MF63 did not cause NSAID-like gastrointestinal toxic effects, such as mucosal erosions or leakage in the KI mice or nonhuman primates, although it markedly inhibited PGE2 synthesis in the KI mouse stomach.

Protocol
Cell Experiment
Cell lines A549 cells
Preparation method A549 cells were seeded in 96-well dishes at a density of 25,000 cells/well and incubated for 20 h in RPMI 1640 medium supplemented with 2% fetal bovine serum (FBS). The cells were then incubated with 10 ng/ml IL-1 for 24 h in the presence of a vehicle or inhibitor from a 100-fold concentrated DMSO stock solution in a medium containing 2 or 50% FBS. Concentrations of PGE2 and PGF2 in the cell-free medium were measured by EIA (Assay Designs Inc.). IC50 values were derived from eight-point titrations.
Concentrations 0.01~100 µ M
Incubation time 24 h
Animal Experiment
Animal models mPGES-1 Knock-In Mice
Formulation a suspension in 0.5% methylcellulose
Dosages 100 mg/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 378.81
Formula C23H11ClN4
CAS Number 892549-43-8
Purity 99.59%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Oncotarget (2016). Figure 4. MF63 (Abmole Bioscience, Houston, TX, USA)
Method
Cell Lines mPGES-1+/+ cells
Concentrations 10 μM
Incubation Time 18 h
Results Moreover, MF63 increased levels of both miRs in mPGES-1+/+ cells (Figure 4C), and miR-15a and miR-186 were up-regulated with respect to mPGES-1+/+ tumors in DU145 mPGES-1-/- xenografts in vivo (Figure 4D).
Rating
Source Oncotarget (2016). Figure 3. MF63 (Abmole Bioscience, Houston, TX, USA)
Method
Cell Lines mPGES-1+/+ cells
Concentrations 10 μM
Incubation Time
Results Consistently,MF63 (10 μM) significantly increased Dicer expression in mPGES-1+/+ cells (Figure 3B), whereas exogenous PGE-2(1 μM, 2–24 h) decreased in mPGES-1-/- cells (Figure 3C).
Rating
Source Oncotarget (2016). Figure 1. MF63 (Abmole Bioscience, Houston, TX, USA)
Method
Cell Lines mPGES-1+/+ cells
Concentrations 10 μM
Incubation Time
Results MF63 (10 μM), a reversible mPGES-1 inhibitor, significantly decreased VEGF expression in mPGES-1+/+ cells with maximum effect at 8–18 h (Figure 1D), while exogenous PGE-2 (1 μM) increased VEGF release and expression in mPGES-1-/- cells time-dependently (Figure 1B, 1E).
Rating
Source Am J Physiol Gastrointest Liver Physiol (2016) . Figure 4.mPGES-1 inhibitor MF63 (Abmole bioscience, Houston, TX)
Method Western blotting analysis
Cell Lines
Concentrations 1µM
Incubation Time 6 h
Results The above effects were attenuated by pretreatment with the mPGES-1 inhibitor, MF63, in Jo2-treated mPGES-1 Tg mice (Fig. 4A). These findings indicate an important role of EGFR/Akt and associated apoptosis-regulatory molecules in mPGES-1-mediated protection against liver injury.
Rating
Source Am J Physiol Gastrointest Liver Physiol (2016) . Figure 1.mPGES-1 inhibitor MF63 (Abmole bioscience, Houston, TX)
Method mPGES-1 Tg mice oral gavage (twice every 12 h)
Cell Lines
Concentrations 50µg/g body weight
Incubation Time 5 h
Results Two doses of MF63 were administrated via oral gavage (every 12h) before Jo2 injection and the mice were sacrificed 5 hours after Jo2 injection (outlined in Fig. 3A). We observed that MF63 pretreatment partially reversed the resistance of mPGES-1 Tg mice to Jo2-induced liver injury (Fig. 3B-F).These findings further support the role of mPGES-1 in modulation of Fas-induced hepatocyte apoptosis and liver injury.
Rating
Source Endocrinology (2015) . Figure 4. MF63 was from AbMole.
Method EIA assay and western blot analysis
Cell Lines DU145, PC-3
Concentrations 10 µ M
Incubation Time 48 h
Results MF63 (10 µmol l-1, 24-48 h) significantly inhibited PGE2 production and reversed the mesenchymal phenotype in DU145 and PC-3 cells, promoting E-cadherin and inhibiting vimentin expression (Fig. 4A, B and C). MF63 also upregulated α6-integrin and significantly reduced cell clonogenicity (Fig.4D, and E).
Rating
Product Citations
References

MF63 [2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile], a selective microsomal prostaglandin E synthase-1 inhibitor, relieves pyresis and pain in preclinical models of inflammation.
Xu et al. J Pharmacol Exp Ther. 2008 Sep;326(3):754-63. PMID: 18524979.

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Keywords: MF63 supplier, PGE synthase, inhibitors

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