ionophore

Calcium Ionophore I has a wide range of applications in life science related research.

Sodium ionophore III (ETH2120) is a Na+ ionophore suitable for the test of sodium activity in plasma, serum, and blood.

Calcium ionophore II (N,N,N′,N′-Tetracyclohexyl-3-oxapentanediamide) is a lipophilic ionophore that can be used in preparing calcium ion-selective electrode.

Lasalocid (Lasalocid-A) is an ion carrier antibiotic produced by Streptomyces, which has antimicrobial and parasitic properties and is often added to feed.

Lasalocid sodium (Lasalocid-A sodium) is a cationic ionophore antibiotic obtained from Streptomyces lasaliensis that, among other effects, dissociates the calcium fluxes in muscle fibers. Lasalocid sodium is used as a coccidiostat, especially in poultry.

Elesclomol (STA-4783) is an oxidative stress inducer and a highly lipophilic copper ion carrier. Elesclomol induces apoptosis in tumor cells and is used in copper death related studies. Elesclomol also inhibits FDX1-mediated Fe-S cluster biosynthesis.

Ionomycin is an calcium ionophore and an antibiotic that binds calcium ions (Ca2+). It is produced by the bacterium Streptomyces conglobatus.It is used in research to raise the intracellular calcium level (Ca2+) and as a research tool to understand Ca2+ transport across biological membranes. Ionomycin promotes apoptosis and induces the activation of protein kinase C (PKC).

lonomycin calcium is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. also induces the activation of protein kinase C (PKC). Ionomycin calcium (SQ23377 calcium) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin promotes apoptosis.

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid. It is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Moreover, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. Given its diverse applications, AACOCF3 holds promise for cardiovascular disease research.

Nigericin is an antibiotic derived from Streptomyces hygroscopicus that acts as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes. Nigericin can be an NLRP3 activator that causes the release of IL-1β as a NALP3-dependent manner. N

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.

Semduramicin sodium is a carboxylic acid ionophore for management of chicken coccidiosis.

(±)14-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. DHA is metabolized to 14(S)-HDHA by human platelets along with 11(S)-HDHA. 14(S)-HDoHE is also produced by salmon gills upon stimulation with calcium ionophore. 14(S)-HDHA was shown to be an inhibitor of U-46619-induced human platelet aggregation and rabbit and rat aortic smooth muscle contraction with IC50 values of about 70, 3.6, and 5.3 μM, respectively. (±)14-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.

5(S),15(S)-DiHETE is synthesized by 15-LO from 5(S)-HETE. It potentiates the degranulation of human PMNL in response to PAF, but not fMLP, calcium ionophore A23187, or LTB4. 5(S),15(S)-DiHETE is chemotactic for eosinophils with an ED50 value of 0.3 μM.

11-trans Leukotriene C4 (11-trans LTC4) is a C-11 double bond isomer of LTC4. LTC4 undergoes slow temperature-dependent isomerization to 11-trans LTC4 during storage. 11-trans LTC4 is produced in smaller amounts relative to LTC4 in ionophore-stimulated HMC-1 cells (a human mast cell line) and equine eosinophils, but not in human neutrophils or RBL-1 cells. It is nearly equipotent with LTC4 for contraction of guinea pig parenchymal and ileum. In a radioligand binding assay using guinea pig ileum as a cysteinyl leukotriene receptor preparation, the pKis for LTC4 and 11-trans LTC4 were determined to be 6.42 and 6.58, respectively.

5(S),12(S)-DiHETE is a natural bioactive lipid derived from arachidonic acid . It is synthesized by glycogen-induced rabbit peritoneal polymorphonuclear leukocytes (PMNLs) incubated with AA. 5(S),12(S)-DiHETE can be produced by successive oxygenation of AA by 5-lipoxygenase (5-LO) in platelets and 12-LO in leukocytes. It can also be synthesized from 12(S)-HETE by 5-LO, in the presence of 5-LO activating protein (FLAP), activated with calcium ionophore. 5(S),12(S)-DiHETE is an epimer of leukotriene B4 that is weakly chemotactic for PMNL.

Resolvins are a family of potent lipid mediators derived from both eicosapentaenoic acid and docosahexaenoic acid . [1] In addition to being anti-inflammatory, resolvins promote the resolution of the inflammatory response back to a non-inflamed state.[2] Resolvin D5 (RvD5) is a DHA-derived resolvin generated by a double dioxygenation mechanism.[3] RvD5 has been identified in media from ionophore-stimulated trout brain cells, in human synovial fluid from patients with rheumatoid arthritis, and in exudates of bacterial infections in mice. [4][5][6] RvD5 stimulates the phagocytosis of E. coli by human macrophages, and RvD5 methyl ester enhances bacterial killing in mice inoculated with E. coli. [6] Analytical and biological comparisons of synthetic RvD5 with endogenously derived RvD5 have confirmed its identity as matching the natural product.[7]

1,3-Dipalmitoleoyl-rac-glycerol is a diacylglycerol with palmitoleic acid at the sn-1 and sn-3 positions. It selectively inhibits α-glucosidase from S. cerevisiae over rat enzyme (IC50s = 4.45 and 9,326.5 μM, respectively). 1,3-Dipalmitoleoyl-rac-glycerol has been used in the formation of lipid bilayers to study the effects of membrane composition and the ionophore valinomycin on membrane potential.

Glutinone (IC50=24 microM) shows a significant effect on thromboxane B2 (TXB2)-release induced by calcium ionophore in human platelets.

Deethylindanomycin is a polyether antibiotic that has been found in S. setonii. It is active against a variety of Gram-positive bacteria, including various strains of S. aureus and Streptococcus, as well as one strain of S. pneumoniae (MICs = 4, 4, and 2 μg/ml, respectively). It is also active against coccidia in vitro, inhibiting E. tenella development, but is inactive against E. tenella infection in chicks when administered at a dose of 200 μg/g in the diet. Deethylindanomycin acts as an ionophore in lipid bilayer membranes and is more selective for potassium ions than calcium, magnesium, and sodium ions. It induces histamine release from rodent mast cells and human basophils in vitro in a calcium-dependent manner.

Semduramicin is a carboxylic acid ionophore for management of chicken coccidiosis.

U-51605, a stable analog of the endoperoxide prostaglandin H2 (PGH2), functions as an inhibitor with greater selectivity towards prostacyclin (PGI) synthase over thromboxane (TX) synthase. It also acts as a partial agonist at TP receptors. Studies show that at a concentration of 2.8 µM, U-51605 effectively inhibits PGI synthase in human foreskin fibroblasts, while a concentration of 5.6 µM is required to inhibit human platelet TX synthase. Furthermore, U-51605, at up to 1 µM, decreases the release of prostacyclin in SHR aorta triggered by the calcium ionophore A-23187 without impacting TXA2 production, and notably enhances the release of PGE2 and PGF2α.

Calcimycin (A-23187) hemicalcium salt is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). It induces Ca2+-dependent cell death by increasing intracellular calcium concentration.

Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, specifically inhibits the growth of gram-positive bacteria. It acts as a potent inhibitor of Wnt/β-catenin signaling, blocking Wnt-induced LRP6 phosphorylation. Additionally, Salinomycin (Procoxacin) demonstrates selective activity against human cancer stem cells.

GV-196771 selectively antagonize the glycine-binding site of the NMDA ionophore.

Prostaglandin E2 (PGE2) inhibitor 3 is a selective inhibitor targeting microsomal prostaglandin E synthase-1 (mPGES-1; IC50 = 0.2 µM), demonstrating greater selectivity for mPGES-1 over COX-1, COX-2, 5-lipoxygenase (5-LO), and soluble epoxide hydrolase (sEH) in assays at 10 µM. This compound effectively reduces IL-1β-induced PGE2 production in A549 cells and decreases LPS-induced IL-6 and PGE2 in J774A.1 macrophages at concentrations of 10 and 1 µM, respectively. Additionally, it blocks the production of 5-LO-derived products, including leukotriene B4 (LTB4) and 5-H(p)ETE, in response to calcium ionophore A23187 alone or combined with arachidonic acid, with IC50 values of 4.9 and 5.2 µM, respectively. When administered in vivo at doses of 10 mg/kg, PGE2 inhibitor 3 effectively prevents leukocyte infiltration in a mouse model of zymosan-induced peritonitis.

AS-701 is a Li+ selective ionophore in the therapy of manic-depressive illness.

Salinazid (Salicylaldehyde isonicotinoyl hydrazone) is a potent Cu(II) ionophore which preferentially kills HepG2 cells over HUVEC cells, and is superior to clioquinol.

1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE is a phospholipid that contains stearic acid at the sn-1 position and 15(S)-HETE at the sn-2 position. It is formed in human peripheral monocytes activated by the calcium ionophore A23187 by direct oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE by 15-LO. Phosphoethanolamine (PE) HETEs (PE-HETEs), including 1-stearoyl-2-15(S)-HETE-sn-glycero-3-PE, are the main source of esterified HETE in ionophore-activated monocytes.

Calcimycin (A-23187) hemimagnesium, an antibiotic and divalent cation ionophore (such as calcium and magnesium), serves various biological roles. It triggers Ca2+-dependent cell death by elevating intracellular calcium levels and suppresses the growth of Gram-positive bacteria and certain fungi. Additionally, this compound hinders ATPase activity and uncouples oxidative phosphorylation (OXPHOS) in mammalian cells, ultimately leading to apoptosis [1] [2] [3] [4].

Salinomycin sodium salt (Sodium salinomycin), an antibiotic potassium ionophore, is an effective inhibitor of Wnt/β-catenin signaling.

AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively. IC50 value: 2.2 nM/0.6 nM/154 nM(FLAP binding/hLA/hWB) [1] AM679 showed an improved CYP inhibition profile (IC50 3A4 = 16.7 lM, 2C9 =

LY255283 is a specific antagonit of leukotriene B4 (LTB4) receptor. It inhibits the production of LTB(4) in human peripheral blood polymorphonuclear leukocytes (PMNL) and in monocytes activated by calcium ionophore A23187.

Lipoxygenin is an inhibitor of 5-lipoxygenase (5-LO) with an IC50value of 5 μM for inhibition of 5-LO product synthesis in isolated human granulocytes stimulated with the cation ionophore A23187 .1It inhibits hedgehog-dependent signaling in Shh-LIGHT2 cells and TGF-β-, activin A-, bone morphogenic protein (BMP)-, or Wnt-dependent signaling in HEK293T cells (IC50s = 9.3, 3.2, 8.2, 9.6, and 3.7 μM, respectively, in luciferase reporter assays). Lipoxygenin (5 and 10 μM) increases levels of troponin T (TnnT), a marker of cardiomyocyte differentiation, in human induced pluripotent stem cells (iPSCs) stimulated with BMP4 and the glycogen synthase kinase 3 (GSK3) inhibitor CHIR99021 .

4-Bromo A23187 is a halogenated analog of the calcium ionophore A-23187. 4-Bromo A23187 is a calcium modulator and induces apoptosis in different cells.

A 55453 is a radiated ionophore used as a reversibl, high-affinity alpha 1-adrenergic receptor probe.

Enniatin C is an ionophore that can bind ammonium.

Nesiritide, a 32-amino acid natriuretic peptide and recombinant form of human brain natriuretic peptide, enhances vasorelaxation ex vivo in porcine hearts from an acute coronary occlusion model when given as a 2 µg/kg bolus dose followed by a 0.01 µg/kg per minute infusion, facilitated by the calcium ionophore A23187. Formulations containing nesiritide have been utilized in managing congestive heart failure.

Calcimycin (A-23187) is an ionophorous, polyether carboxylic antibiotic from Streptomyces chartreusensis. It binds and transports calcium and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems.

Morolic acid and moronic acid have shown sustained antidiabetic and antihyperglycemic action possibly mediated by an insulin sensitization with consequent changes of glucose, cholesterol and triglycerides, in part mediated by inhibition of 11β-HSD 1. Moro

Tetranactin is a macrotetrolide and a monovalent cation ionophore that has been found in S. aureus and has antibacterial, insecticidal, and mitogenic activities. It exhibits an equilibrium permeability ratio 1,000-fold greater for lithium than sodium or cesium ions accross bilayer membranes at low voltages. Tetranactin inhibits the growth of Gram-positive bacteria and C. miyabeanus and R. solani fungi when used at concentrations less than 0.9 μg/ml. Tetranactin (0.5-1.5 μg per insect) dose-dependently increases the mortality of adult C. chinensis weevils up to 100% and has mitogenic activity against T. telarius when sprayed onto plants with an LC50 value of 9.2 μg/ml. It reduces IL-1β- and cAMP-induced secretion of phospholipase A2 (PLA2) from rat mesangial cells (IC50s = 43 and 33 nM, respectively). Tetranactin (50 ng/ml) suppresses the proliferation of human T lymphocytes induced by allogeneic cells and IL-2 and supresses the generation of cytotoxic T lymphocytes in mixed lymphocyte cultures. In vivo, tetranactin (10 mg/animal per day) completely inhibits the formation of experimental autoimmune uveoretinitis (EAU) in rats.

A28086B is an ionophore antibiotic.

UK 58852 is a polyether ionophore.

Pyrithione (1-hydroxyl-1H-pyridine-2-thione) is a transition metal complex, a zinc ionophore, that causes elevated zinc levels in mammalian cells. Pyrithione has potent bactericidal and antifungal activity.

Laidlomycin butyrate is a ionophore with enhanced intraruminal activity.