PF-9184
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PF-9184 is a novel mPGES-1 inhibitor [1]. Microsomal prostaglandin E synthase-1 (mPGES-1) is an inducible terminal isomerase expressed in cytokine-sensitive brain endothelial cells. mPGES-1 functions as the central switch during immune-induced pyresis and as a target for treatment of fever and other PGE2-dependent acute phase reactions elicited by the brain [2]. mPGES-1 has been incolved in the formation of PGE2 essential for pain hypersensitivity and inflammation. Microsomal prostaglandin E synthase-1 (mPGES-1) has been involved in converting the COX product prostaglandin H2 (PGH2) into the biologically active PGE2[3].
In vitro: PF-9184 potently inhibited recombinant human mPGES-1 with an IC50 value of 16.5 ± 3.8 nM. PF-9184 showed no effect on rhCOX-1 and rhCOX-2 with >6500-fold selectivity. In rationally designed cell systems, PF-9184 inhibited PGE2 synthesis with IC50 in the range of 0.5–5 μM in serum-free cell and human whole blood cultures, while sparing the synthesis of 6-keto-PGF1α (PGF1α) and PGF2α[1]. PF-9184 showed no apparent cytotoxic effects up to 100 μM [1].
References:
[1] Mbalaviele G, Pauley A M, Shaffer A F, et al. Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor[J]. Biochemical pharmacology, 2010, 79(10): 1445-1454.
[2] Engblom D, Saha S, Engstrm L, et al. Microsomal prostaglandin E synthase-1 is the central switch during immune-induced pyresis[J]. Nature neuroscience, 2003, 6(11): 1137-1138.
[3] Jakobsson P J, Thorén S, Morgenstern R, et al. Identification of human prostaglandin E synthase: a microsomal, glutathione-dependent, inducible enzyme, constituting a potential novel drug target[J]. Proceedings of the National Academy of Sciences, 1999, 96(13): 7220-7225.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 461.3 |
Cas No. | 1221971-47-6 |
Formula | C21H14Cl2N2O4S |
Solubility | ≤15mg/ml in DMSO;20mg/ml in dimethyl formamide |
Chemical Name | N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide |
SDF | Download SDF |
Canonical SMILES | OC1=C(C(NC2=CC=C(C3=CC=C(Cl)C(Cl)=C3)C=C2)=O)NS(C4=CC=CC=C41)(=O)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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