Activators & Inhibitors

Pyridindolol (Legacy Tebubio ref. 282T37330). Pyrindolol is a bacterial metabolite that has been found inS. alboverticillatus.1It inhibits neutral β-galactosidase by 50% under acidic, but not neutral, conditions when used at a concentration of 2 μg/ml. It is selective for β-galactosidase isolated from bovine liver over β-galactosidases isolated from human, bovine, pig, and rat tissues and sialidases isolated fromC. perfringens,Streptomyces, and the H3N2 strain of influenza virus (IC50s = >250 μg/ml for all).1,2

Pyrrophenone (Legacy Tebubio ref. 282T37331). The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs). Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively). Its action is reversible and selective, as pyrrophenone inhibits the secretory type IB and IIA PLA2s with more than a hundred-fold less potency. Pyrrophenone has also been shown to inhibit calcium ionophore (A23187)-stimulated AA release from monocytic cells, interleukin-1-induced PGE2 synthesis in mesangial cells, and the production of PGE2, LTs, and platelet-activating factor by human neutrophils, always with maximal inhibition at concentrations below 1 μM.

(±)-N-3-Benzylnirvanol (Legacy Tebubio ref. 282T37332). (±)-N-3-Benzylnirvanol is a racemic mixture of (+)-N-3-Benzylnirvanol and (-)-N-3-Benzylnirvanol. Both enantiomers are selective inhibitors of cytochrome P450, specifically inhibiting CYP2C19. (±)-N-3-Benzylnirvanol also reduces plasma cholesterol levels in mice.

(±)11,12-DiHETE (Legacy Tebubio ref. 282T37334). (±)11,12-DiHETE is a dihydroxy metabolite of EPA produced by cytochrome P450-mediated epoxide formation and subsequent hydrolysis by epoxide hydrolase. Plasma levels of (±)11,12-DiHETE are increased over baseline after an oral dose of 1008 mg EPA.

3-Hydroxy-C4-HSL (Legacy Tebubio ref. 282T37335). 3-Hydroxy-C4-HSL (N-3-hydroxybutyryl-L-Homoserine lactone) is an N-acyl homoserine lactone obtained from pathogenic Vibrio vulnificus in fish and is a bacterial group sensing (QS) inducer that modulates bacterial signaling and can be used in the study of bacterial infections.

3-Oxo-C16:1 (Legacy Tebubio ref. 282T37336). 3-Oxo-C16:1-HSL (3oxoC16:1Δ11cis(L)HSL) is an N-acyl-homoserine lactone from Pseudomonas aeruginosa that inhibits the pathogenic strains of Aspergillus vinelandii from causing crown galls on grapes, and can be used in biosensor research.

N-3-oxo-hexadecanoyl-L-Homoserine lactone (Legacy Tebubio ref. 282T37337). N-3-oxo-hexadecanoyl-L-Homoserine lactone is an unusual, substituted, long-chain N-acyl-homoserine lactone (AHL) produced by some bacteria, including strains of Agrobacterium vitis and Pseudomonas. Like other AHLs, this C16-containing form is thought to be involved in quorum sensing. Substituted, long-chain AHLs, including N-3-oxo-tetradecanoyl-L-homoserine lactone , prime for systemic acquired resistance to pathogen attack in plants.

N-3-oxo-pentanoyl-L-Homoserine lactone (Legacy Tebubio ref. 282T37338). N-3-oxo-pentanoyl-L-Homoserine lactone is a chain-shortened derivative of the bacterial quorum sensing signaling molecule N-3-oxo-octanoyl-L-homoserine lactone .1It inhibits binding of the autoinducer N-3-oxo-hexanoyl homoserine lactone toE. colicontaining the transcription factor LuxR when used at a concentration of 230 nM.2It acts as an autoinducer to activate theV. fischeriluminescence system inE. coliwhen used at concentrations ranging from 20 to 200 nM.

N-3-oxo-tetradecanoyl-L-Homoserine lactone (Legacy Tebubio ref. 282T37339). Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density. Controlling bacterial infections by quenching their quorum sensing systems is a promising field of study. The expression of specific target genes, such as transcriptional regulators belonging to the LuxIR family of proteins, is coordinated by the synthesis of diffusible acylhomoserine lactone (AHL) molecules. N-3-oxo-tetradecanoyl-L-homoserine lactone (3-oxo-C14-HSL) is a small diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and affecting cellular metabolism in bacteria.[1] [2] [3] It appears later than shorter acyl chain AHLs in developing biofilms [4] and, like other long chain 3-oxo-AHLs, stimulates the production of putisolvin, [5] which in turn, inhibits biofilm formation.