rbl-2h3 cells

MK-571 sodium (L-660711 sodium salt) is a selective, orally active antagonist of the CysLT1 receptor. MK-571 sodium is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor used to demonstrate the role of Mrp2 in the cellular efflux of drugs, xenobiotics, and their conjugates. MK-571 sodium can inhibit the synthesis of K-4′-O-GlcA (19.7 μM). MK571 dose-dependently inhibits the intracellular biosynthesis of all flavonol sulphates and glucuronides by Caco-2 cells. MK-571 sodium significantly inhibits phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and production of kaempferol-4′-O-glucuronide was competitively inhibited. In addition to inhibiting MRP2, MK571 is a potent inhibitor of enterocyte phase-2 conjugation.

Linoleic acid (9,12-octadecadienoic acid) is a naturally occurring polyunsaturated fatty acid found in animal and vegetable oils. Linoleic acid is an essential fatty acid that is part of membrane phospholipids.

Eicosapentaenoic Acid is an ω-3 fatty acid and an inhibitor of fatty acid synthase (FASN). Eicosapentaenoic Acid promotes DNA demethylation in the reexpression of the tumor suppressor gene CCAAT/ enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates the RAS/ERK/C/EBPβ pathway in U937 leukemia cells through demethylation of the CpG island of H-RAS intron 1. Eicosapentaenoic Acid promotes the relaxation of vascular smooth muscle cells and vasodilation.

T-5224 is a selective inhibitor of the transcription factor c-Fos/activator protein (AP)-1 with anti-inflammatory effects. T-5224 specifically suppresses the DNA-binding activity of c-Fos/c-Jun, thereby inhibiting IL-1β-induced transcriptional upregulation of Mmp-3, Mmp-13, and Adamts-5, without affecting the binding activity of other transcription factors. T-5224 can be used in research on rheumatoid arthritis, osteoarthritis, and cartilage degeneration.

Ketotifen is a second-generation, orally active, non-competitive histamine 1 (H1) receptor blocker and mast cell stabilizer that inhibits 6-phosphogluconate dehydrogenase (6-PGD) in vitro. Ketotifen exhibits antiviral activity against SARS-CoV-2 and influenza virus and is suitable for research on experimental autoimmune encephalomyelitis (EAE) and asthma attack prevention.

OMDM-1 ((Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide) is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor with a Ki of 2.4 μM.

OMDM-2 is a metabolically stable and selective inhibitor of anandamide cellular uptake (ACU), exhibiting a Ki value of 3.0 μM in RBL-2H3 cells and demonstrating excellent stability during rat brain homogenate digestion.

OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM).

Pyr6 (N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide) is a selective TRPC3 inhibitor with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).Pyr6 is an inhibitor of Ca2+ entry, which displays higher potency to inhibit Ca2+ entry mediated by CRAC channel than by TRPC3.

MRS2690 disodium is a selective agonist of the P2Y14 receptor. It inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and causing concentration-dependent vasoconstriction in porcine coronary arteries. MRS2690 disodium induces intracellular calcium mobilization, activates P38, and stimulates [35S]GTPγS binding on the membrane of RBL-2H3 cells. It also enhances the β-hexosaminidase (β-Hex) release induced by antigen (NP-BSA) and C3a. This compound is useful for research in ischemic heart disease.

SB 204900 inhibit the release of histamine and TNF-α from RBL-2H3 cells.

Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has diverse biological activities, including antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 20 μM. Streptochlorin (12 μg/ml) decreases viability of, as well as induces apoptosis and increases the production of reactive oxygen species (ROS) in, Hep3B human hepatocellular carcinoma cells. It does not induce cytotoxicity in RBL-2H3 mast cells at concentrations up to 100 μM. Streptochlorin prevents degranulation in antigen-stimulated mast cells, as well as inhibits Syk kinase and the Src family kinases LYN and Fyn and reduces the secretion of TNF-α and IL-4 induced by dinitrophenyl-human serum album (DNP-HSA) in RBL-2H3 mast cells. It also decreases swelling and reduces scratching behavior in a mouse model of allergic dermatitis induced by dinitrofluorobenzene (DNFB).

9(S),12(S),13(S)-TriHOME is a linoleic acid-derived oxylipin that has diverse biological activities.1,2,3,4It has been found in various plants and is produced in human eosinophils in a 15-lipoxygenase-dependent, soluble epoxide hydrolase-independent manner.1,59(S),12(S)13(S)-TriHOME inhibits antigen-induced β-hexosaminidase release from RBL-2H3 mast cells (IC50= 28.7 μg/ml).2It inhibits LPS-induced nitric oxide (NO) production in BV-2 microglia (IC50= 40.95 μM).3In vivo, 9(S),12(S),13(S)-TriHOME (1 g/animal) enhances the antiviral IgA and IgG antibody responses induced by a nasal influenza hemagglutinin (HA) vaccine by 5.2- and 2-fold, respectively, in mice.4 1.Hamberg, M., and Hamberg, G.Peroxygenase-catalyzed fatty acid epoxidation in cereal seeds: Sequential oxidation of linoleic acid into 9(S),12(S),13(S)-trihydroxy-10(E)-octadecenoic acidPlant Physiol.110(3)807-815(1996) 2.Hong, S.S., and Oh, J.S.Inhibitors of antigen-induced degranulation of RBL-2H3 cells isolated from wheat branJ. Korean Soc. Appl. Biol. Chem.5569-74(2012) 3.Kim, C.S., Kwon, O.W., Kim, S.Y., et al.Five new oxylipins from Chaenomeles sinensisLipids49(11)1151-1159(2014) 4.Shirahata, T., Sunazuka, T., Yoshida, K., et al.Total synthesis, elucidation of absolute stereochemistry, and adjuvant activity of trihydroxy fatty acidsTetrahedron62(40)9483-9496(2006) 5.Fuchs, D., Tang, X., Johnsson, A.-K., et al.Eosinophils synthesize trihydroxyoctadecenoic acids (TriHOMEs) via a 15-lipoxygenase dependent processBiochim. Biophys. Acta Mol. Cell Biol. Lipids1865(4)158611(2020)

pNPS-DHA is an arylamide derivative of docosahexaenoyl ethanolamide that has anti-allergic activity.1It inhibits degranulation of RBL-2H3 mast cells (IC50= 15 μM).pNPS-DHA (1,000 mg/kg) inhibits IgE-dependent passive cutaneous anaphylaxis (PCA) in mice. 1.Kim, I.-H., Kanayama, Y., Nishiwaki, H., et al.Structure-activity relationships of fish oil derivatives with anti-allergic activity in vitro and in vivoJ. Med. Chem.62(21)9576-9592(2019)

Licochalcone D may be a potential drug for human melanoma treatment by inhibiting proliferation, inducing apoptosis via the mitochondrial pathway and blocking cell migration and invasion. Licochalcone D has cardioprotective potential against myocardial is

Variegatic acid is a natural inhibitor of β-hexosaminidase release and tumor necrosis factor (TNF)-α secretion from rat basophilic leukemia (RBL 2H3) cells, with IC50 values of 10.4 μM and 16.8 μM, respectively, also inhibiting PKC β1 activity with an IC50 value of 36.2 μM.

Licochalcone C (LICOCHALCONEC) has potent antioxidant properties and inhibition of bacterial growth and cellular respiration. It has cardioprotection effect, via antioxidant, anti-inflammatory, and anti-apoptotic activities. Licochalcone C exhibit inhibitory activity with cytotoxicity in a rat basophilic leukaemia cell line, RBL-2H3. Licochalcone C induces apoptosis via B-cell lymphoma 2 family proteins in T24 cells, it may be a potential adjuvant therapeutic agent for bladder cancer.

Maceneolignan A, a natural product isolated from the aril of Myristica fragrans (Myristicaceae), inhibits β-hexosaminidase release in RBL-2H3 cells, exhibiting an IC50 of 48.4 μM. Additionally, it suppresses TNF-α release in antigen-stimulated RBL-2H3 cells with an IC50 of 63.7 μM [1].

Procyanidin A1 (Standard) is a reference standard for research and analysis in studies involving Procyanidin A1. Procyanidin A1 (Proanthocyanidin A1) has antiallergic effects, it inhibits degranulation downstream of protein kinase C activation or Ca2+; influx from an internal store in RBL-2H3 cells.

Procyanidin A1 (Proanthocyanidin A1) has antiallergic effects, it inhibits degranulation downstream of protein kinase C activation or Ca2+; influx from an internal store in RBL-2H3 cells.

Dichotomine C ((R)-(-)-Dichotomine C) is a β-carboline alkaloid with anti-allergic properties. It inhibits the release of β-hexosaminidase from RBL-2H3 cells with an IC50 of 62 μM. Additionally, it suppresses antigen IgE-mediated release of TNF-α and IL-4 in RBL-2H3 cells, with IC50 values of 19 μM and 15 μM, respectively. This compound is applicable in the research of type I hypersensitivity reactions.

25R-Inokosterone exhibits potent inhibition against TNF-expression levels in A23187 plus phorbol-myrisrate acetate-induced RBL-2H3 cells. 25R-Inokosterone has excellent anti-atopy activity, thus 25R-Inokosterone could be used to a large range of functional anti-atopy cosmetics.

25S-Inokosterone is a plant ecdysosteroid isolated from the roots of Achyranthes bidentata. 25S-Inokosterone shows potential for use in studies of LPS-induced acute kidney injury.

Kushenol N may have anti-allergic activity, it demonstrates significant inhibition of the release of beta-hexosaminidase from cultured RBL-2H3 cells .