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Myeloperoxidase (MPO), released from neutrophils to degrade invading pathogens, provides one of the earliest lines of defense in innate immunity. It catalyzes the hydrogen peroxide-mediated oxidation of halide ions to products such as hypochlorous acid (HOCl). These reactive products participate in...
A β-lactam antibiotic in the cephalosporin class.
A DHA metabolite, also referred to as protectin DX (PDX), produced by an apparent double lipoxygenase-mediated reaction; blocks neutrophil infiltration in mouse peritonitis by 20-25% at a dose of 1 ng/mouse; inhibits platelet activation by both impairing TX synthesis and TX receptor activation.
A progesterone analog (i.e., a progestin); does not bind the ER, however, two of its A-ring metabolites can bind ER and possess weak estrogenic activity.
Troglitazone is a TZD which was approved for the treatment of insulin resistance and hyperglycemia in Type II diabetes, under the trade name Resulin™, but was withdrawn from the market due to hepatotoxicity. Troglitazone is a potent and selective PPARγ agonist. The EC50 values...
15(R)-HETE is produced when aspirin-inhibited COX-2 is incubated with arachidonic acid. The clinical significance of 15(R)-HETE and its potential downstream metabolites is the subject of current investigations.
Formal Name: N-[3-chloro-4-[[(2-chlorophenyl)amino]sulfonyl]phenyl]-2-pyridinecarboxamide CAS Number: 1246086-78-1 Molecular Formula: C18H13Cl2N3O3S Formula Weight: 422.3
This nuclear receptor assay system utilizes proprietary non-human cells engineered to provide constitutive, high-level expression of the human retinoic acid receptor gamma (NR1B3), a ligand-dependent transcription factor commonly referred to as RARG or RARγ. INDIGO’s reporter cells...
Has the fluorophore NBD attached to the ω-end of the stearoyl chain of SAG; may be used to study interactions with proteins, utilization by cells and liposomes, and for the development of assays for lipid metabolism.
The PLAs are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components. The iPLA2 are a PLA2 subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (S)-BEL is an irreversible,...
A synthetic analog of natural PtdIns containing C8:0 fatty acids at the sn-1 and sn-2 positions; contains the same inositol and DAG stereochemistry as the natural compound.
A phospholipid abundant in the inner leaflet of the plasma membrane that interacts with cholesterol to form a condensed lipid monolayer that facilitates transport and signaling across the bilayer.
A thyroid hormone that is about 1,000-fold less active at the thyroid hormone receptors TRα and TRβ than T3; activates TRΔα1, a native form of TRα that lacks a nuclear localization signal and functions in the cytoplasm, initiating actin polymerization.
BS-181 is a Cdk7 inhibitor that blocks the activity of Cdk-activating kinase with an IC50 value of 21 nM.1 It inhibits Cdk2 at a concentration 35-fold higher than that of Cdk7. BS-181 has been shown to inhibit the phosphorylation of Cdk7 substrates, to promote cell cycle arrest and...
A tetracycline-like antibiotic which effectively controls or prevents a diverse array of infections; used as the regulator for inducible gene expression systems; inhibits certain MMPs, such as MMP-8 (Ki = 36 µM).
A pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis; widely used to treat many gastrointestinal tract adenocarcinomas.
A prodrug of the ACE inhibitor, temocaprilat (IC50 = 3.6 and 7.6 nM in isolated rat lung and aorta, respectively); used to reduce blood pressure, improve endothelial dysfunction, and prevent vascular remodeling, as well as improve insulin sensitivity and renal function in certain...
A small diffusible signaling molecule involoved in quorum sensing, controlling gene expression, and affecting cellular metabolism; applications of this molecule include infection prevention and a regulation of virulence in general and in cystic fibrosis.
An epimer of chlortetracycline.
A channel blocker that acts on several TRP channels, including TRPM2, TRPM8, and TRPC6 (IC50 = 1.7, 3.8, and 2.3 μM, respectively); inhibits PLA2, blocking the release of arachidonic acid when given at 50 μM.
Tris-glycine stock solution (10X) contains filtered Tris-base containing 1.9 M glycine.
A synthetic analog of natural AHLs that suppresses host immunity without inducing LasR; inhibits the proliferation of mouse peripheral blood leukocytes by concanavalin A (EC50 = 9.3 μM) without concurrent cytotoxicity; does not induce LasR at 100 μM.