Activators & Inhibitors

Aureusimine B (Legacy Tebubio ref. 282T37753). Aureusimine B, a Calpain inhibitor, is produced by Staphylococcus aureus biofilms and could be a potential biomarker for S. aureus biofilm-based infections.

Avilamycin A (Legacy Tebubio ref. 282T37754). Avilamycin A is an antibiotic.1 It is active against veterinary isolates of C. perfringens (MICs = ≤0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml).1,2 Dietary administration of avilamycin A (15 and 30 ppm) reduces mortality in a broiler cockerel model of C. perfringens infection.3 Formulations containing avilamycin A have been used in the prevention of necrotic enteritis in livestock.

Phenylacetyl-Coenzyme A (sodium salt) (Legacy Tebubio ref. 282T37755). Phenylacetyl-coenzyme A (CoA) is a key intermediate in aerobic catabolism of phenylacetate in bacteria such asPseudomonas, when cultured in minimal media using phenylacetate as the sole carbon source.1It is a precursor in the synthesis of the antibiotic penicillin G found in industrial strains ofP. chrysogenum. Phenylacetyl-CoA also acts as an effector molecule of the TetR family transcriptional repressor PaaR inT. thermophilusand the GntR family transcriptional regulator PaaX inE. coliandPseudomonas, binding to each protein to induce derepression of various genes.2

Phloxine B (Legacy Tebubio ref. 282T37756). Phloxine B is a red dye, the USP grade of which is used as a color additive for food, drugs, and cosmetics. It has also been used as an alternative to Gram staining, to differentiate between Gram-negative and Gram-positive bacteria. At 100 μg/ml, it can inhibit methicillin-resistant S. aureus growth in vitro. Phloxine B has also been shown to modulate channel activity of wild-type cystic fibrosis transmembrane conductance regulator chloride channels (CFTR; Ki = 38 μM) and mutant delta F508 CFTR (Ki = 33 μM).

Tyvelose (Legacy Tebubio ref. 282T37757). Tyvelose is an unusual 3,6-dideoxyhexose terminal sugar and the immunodominant component of glycoprotein antigens in the parasitic helminth T. spiralis, which is responsible for trichinosis in humans. It is produced in high amounts by the infective larva and is immunodominant during the muscle stage of infection. Mice immunized with tyvelose-BSA produce IgG1 antibodies to tyvelose but are not resistant to infection by T. spiralis. Tyvelose-specific antibodies (2.5 mg/20 g) administered to rat pups leads to expulsion of first stage larvae from the intestine within one hour.

Unguinol (Legacy Tebubio ref. 282T37758). Unguinol, a depsidone originally isolated from A. unguis, is an inhibitor of pyruvate phosphate dikinase (PPDK; IC50 = 42.3 μM). It inhibits the growth of plants utilizing C4, but not C3, carbon fixation, and also inhibits the growth of the bacteria S. aureus and V. harveyi (GI50s = 8.7 and 69.5 μM, respectively) and H460, MCF-7, and SF-268 cancer cells (GI50s = 28.2, 50.8, and 44.3 μM, respectively).

Fura-2 (potassium salt) (Legacy Tebubio ref. 282T37759). Fura-2 is a ratiometric fluorescent calcium indicator that can be used to detect calcium in cells. [1] It is a pentacarboxylate that displays excitation maxima of 340 and 380 nm at high and low calcium concentrations, respectively, when the emission is fixed at 510 nm, enabling determination of ratiometric measurements of calcium influx in live cells.

Rhapontigenin (Legacy Tebubio ref. 282T3776). Rhapontigenin (Protigenin) is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50: 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons that act as procarcinogens. Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-cancer activity. At higher concentrations, rhapontigenin inhibits the proliferation of HL-60R and HepG2 cancer cell lines (IC50: 48 μM).

Fura-2 (sodium salt) (Legacy Tebubio ref. 282T37760). Fura-2 is a ratiometric fluorescent calcium indicator that can be used to detect calcium in cells. It is a pentacarboxylate that displays excitation maxima of 340 and 380 nm at high and low calcium concentrations, respectively, when the emission is fixed at 510 nm, enabling determination of ratiometric measurements of calcium influx in live cells.