Activators & Inhibitors

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.

Fura-FF pentapotassium salt (Legacy Tebubio ref. 282T37761). Fura-FF pentapotassium salt is a low affinity calcium fluorescent dye (Ex/Em: 365/514 nm, no calcium; 339/507 nm, high calcium).

Fura-FF AM (Legacy Tebubio ref. 282T37762). Fura-FF AM is a cell-permeable acetoxymethyl ester of the fluorescence calcium indicator fura-FF (potassium salt). Upon entering cells, it is hydrolyzed by intracellular esterases to produce fura-FF, a difluorinated derivative of the calcium indicator fura-2. Unlike fura-2, fura-FF has negligible magnesium sensitivity, reducing interference from this cation, and a higher calcium dissociation constant (Kd(calcium) = 6 μM for fura-FF and 0.14 μM for fura-2). The spectral properties of fura-FF are similar to those of fura-2, with fura-FF displaying excitation/emission spectra of 365/514 nm in the absence of calcium and shifting to 339/507 nm in the presence of high calcium concentrations. Low affinity calcium dyes, including fura-FF, are preferred for studying compartments with high calcium concentrations, such as mitochondria, or in cell systems with relatively low calcium buffering capacities, such as neuronal dendrites and spines.

BTD (Legacy Tebubio ref. 282T37763). Selective TRPC5 activator (EC50 = 1.4 μM in a calcium influx assay, 1.3 μM in whole cell patch clamp assay). Displays >14.5-fold selectivity for TRPC5 over other TRP channels (EC50 = 20.6 μM for TRPM8). Also activates TRPC1:5 and TRPC4:5 heteromers.

Cal Green™ 1 (potassium salt) (Legacy Tebubio ref. 282T37764). Cal Green 1 is a cell-impermeant fluorescent calcium indicator that is characterized by high quantum yield and low phototoxicity. Its peak excitation and emission wavelengths (506 and 531 nm, respectively) are comparable to standard fluorescein dyes, making Cal Green 1 appropriate for fluorescent microscopy. Cal Green 1 is ~5-fold brighter than fluo-3 at saturating calcium levels.

Transdermal Peptide (TD 1 (peptide)) (Legacy Tebubio ref. 282T37766). Transdermal Peptide is a 11-amino acid peptide, binds to Na+/K+-ATPase beta-subunit (ATP1B1), and enhances the transdermal delivery of many macromolecules.