phagocytosis

DO-264 is an inhibitor of autohydrolase structural domain 12 (ABHD12) (IC50: 11 nM) and an inhibitor of cellular LysoPS degradation that enhances LPS-induced phagocytosis.

NCGC00135472 (DRV1 (GPR32) agonist C2A) is a human Resolvin DI receptor DRV1 agonist with pro-catabolic properties that activates the human soluble protein D1 receptor DRV1 GPR32 receptor in beta-blocker and cAMP assays with EC50s of 0.37 uM and 0.05 uM, respectively.NCGC00135472 induces in cells overexpressing recombinant DRV1 rapid impedance changes that stimulate phagocytosis of serum-treated zymoglycans.

Boc-Asp(OMe)-fluoromethyl ketone (Boc-Asp(OMe)-FMK) is a broad range caspase inhibitor. Boc-Asp(OME)-Fluoromethyl Ketone inhibits Fas-mediated phagocytosis and oxidative rupture inhibition, but does not affect the chemotactic activity of IL-8.

Traxanox is an orally available diuretic.Traxanox enhances phagocytosis of yeast granules by mouse peritoneal macrophages or rat peritoneal polymorphonuclear leukocytes in vitro.Restorative effect of Traxanox on inhibition of antibody production in BALB c mice.

Traxanox TFA is an orally available diuretic. Traxanox TFA enhances phagocytosis of yeast granules by mouse peritoneal macrophages or rat peritoneal polymorphonuclear leukocytes in vitro. Traxanox TFA restores inhibition of antibody production in BALB c mice. Traxanox TFA is also effective in restoring antibody production in BALB c mice. Traxanox TFA has been shown to enhance phagocytosis in BALB c mice.

Uridine-5'-diphosphate disodium salt (UDP disodium salt) is a specific agonist of the P2Y6 receptors (EC50 = 13 nM for human P2Y6), stimulating the production of inflammatory mediators, phagocytosis, and vasoconstriction. Uridine-5'-diphosphate disodium salt also acts as an antagonist of P2Y14.

O-PHOSPHO-L-SERINE is an ester of serine and phosphate, which are normal metabolites in human biofluids.O-phospho-L-serine is a phagocytosis inhibitor that inhibits glial cell proliferation and cone cell regeneration after photodamage.

L-aspartic acid potasium salt(VX-548) is an amino acid widely found in plants and animals.L-aspartic acid potasium salt drives the production of nitrogen oxides, which promotes phagocytosis and contributes to fish survival.L-aspartic acid potasium salt may stimulate antibiotics. The stimulatory effect may be related to precursors involved in aspartic acid-4-semialdehyde biosynthesis.

Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt β-catenin pathway, and inhibits LPS induction of iNOS expression [3].

ZIM, a norbornene derivative of 4-Aminoantipyrine, effectively induces DNA damage, leading to genomic and chromosomal alterations, cell death, and phagocytosis activation. Its properties highlight its potential as a chemotherapeutic agent in cancer research.

Resolvin D1 (RvD1) is an endogenous pro-inflammatory mediator that blocks pro-inflammatory neutrophil migration by regulating actin polymerization, reduces TNF-α-mediated inflammation in macrophages, and enhances macrophage phagocytosis of apoptotic cells.

RP-182-PEG3-K palmitic acid (Compound 1a) exhibits antitumor activity in mouse B16 melanoma syngeneic grafts and can inhibit CD206highM2-like macrophages (IC50 = 3.2 µM) while inducing phagocytosis.

PLD-IN-1 (Compound 3r) is an orally effective inhibitor of phospholipase D (phospholipaseD) with an IC50 of 1.97 μM. It reduces the expression of CD24, CD47, and PD-L1 while enhancing the expression of calreticulin, thereby modulating the immune evasion mechanisms of lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the viability of lung cancer cell lines A549, HCC44, H460, and HCC15 with IC50 values of 18.44, 22.31, 24.85, and 21.45 μM, respectively. It induces apoptosis (apoptosis) in A549 cells and inhibits cell migration. Additionally, PLD-IN-1 increases pro-inflammatory M1 macrophage levels and decreases anti-inflammatory M2 macrophage levels, exhibiting anti-tumor activity in mouse models.

KB-208 is a phagocytosis inhibitor that enhances immune thrombocytopenia (ITP) in mouse models at a dosage of 1 mg kg. It does not alter other blood parameters or increase serum toxicity biomarkers and is applicable for research in the field of immunology.

ICD inducer-1 (Compound Re1) is an effective inducer of immunogenic cell death (ICD), targeting the endoplasmic reticulum (ER) and subsequently inhibiting ER phagocytosis. It shows promise for cancer research.

Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit

Traxanox sodium is an orally available diuretic. Traxanox sodium enhances phagocytosis of yeast granules by mouse peritoneal macrophages or rat peritoneal polymorphonuclear leukocytes in vitro. Traxanox sodium restores inhibition of antibody production in BALB c mice. Traxanox sodium is also effective in restoring antibody production in BALB c mice. Traxanox sodium has been shown to enhance phagocytosis in BALB c mice.

Gliotoxin-13C13is intended for use as an internal standard for the quantification of gliotoxin by GC- or LC-MS. Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains ofAspergillusand other fungi with diverse biological activities.1,2,3,4,5,6,7,8It inhibits 20S proteasomal chymotrypsin activity (IC50= 10 μM), blocking the degradation of IκBα and preventing the activation of NF-κB.2,3Gliotoxin induces apoptosis in monocytes and dendritic cells and reduces phagocytosis by neutrophils.4,5It suppresses viral infection by Nipah and Hendra virus in HEK293T cells (IC50s = 149 and 579 nM, respectively).6Under reducing conditions, gliotoxin inhibits leukotriene A4hydrolase epoxide hydrolase activity, but not aminopeptidase activity, and leukotriene B4synthesis in neutrophils and monocytes.7

Resolvin conjugate in tissue regeneration 1 (RCTR1) is a specialized pro-resolving mediator (SPM) biosynthesized from docosahexaenoic acid by isolated human macrophages and apoptotic polymorphonuclear (PMN) neutrophils.1It has been found in human spleen and bone marrow.2RCTR1 is produced via lipoxygenase-mediated oxidation of DHA to 7(S)-8-epoxy-17(S)-HDHA, which is conjugated to glutathione.1,2,3RCTR1 (10 nM) increases phagocytosis ofE. colior apoptotic neutrophils in isolated human monocyte-derived macrophages.2It decreases chemotaxis induced by leukotriene B4in isolated human neutrophils when used at a concentration of 10 nM. RCTR1 (1 and 10 nM) accelerates tissue regeneration in planaria. Intraperitoneal administration of RCTR1 (100 ng/animal) shortens the inflammatory resolution period and decreases inflammatory exudate neutrophil infiltration in a mouse model ofE. coli-induced peritonitis. 1.Dalli, J., Ramon, S., Norris, P.C., et al.Novel proresolving and tissue-regenerative resolvin and protectin sulfido-conjugated pathwaysFASEB J.29(5)2120-2136(2015) 2.de la Rosa, X., Norris, P.C., Chiang, N., et al.Identification and complete stereochemical assignments of the new resolvin conjugates in tissue regeneration in human tissues that stimulate proresolving phagocyte functions and tissue regenerationAm. J. Pathol.188(4)950-966(2018) 3.Rodriguez, A.R., and Spur, B.W.First total synthesis of pro-resolving and tissue-regenerative resolvin sulfido-conjugatesTetrahedron Lett.58(16)1662-1668(2017)

Docosahexaenoic acid is a nutritionally-derived ω-3 fatty acid that is abundant in the brain and the retina and is thought to be important in early development and for therapeutic approaches to inflammatory disorders and cancer. 14(S)-HDHA is an oxygenation product of DHA that serves as a precursor to maresin 1 , an anti-inflammatory, pro-resolving mediator that prevents polymorphonuclear neutrophil (PMN) infiltration and stimulates macrophage phagocytosis. At doses as low as 0.2 ng/mouse 14(S)-HDHA administration resulted in reduced infiltration of PMNs into sites of inflammation.

Maresin conjugates in tissue regeneration 1 (MCTR1) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages at the site of inflammation. DHA is oxidized to maresin 1 , which is then converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase. MCTR1 accelerates tissue regeneration in planaria (1 and 100 nM). Pretreatment with MCTR1 (50 ng/mouse, i.p.) prior to E. coli administration reduces neutrophil infiltration, shortens the inflammatory resolution period, and increases phagocytosis of E. coli by macrophages. When administered at a dose of 100 ng 12h post E. coli infection in a mouse model of peritonitis, MCTR1 reduces the amount of eicosanoids in the exudate.

Maresin conjugates in tissue regeneration 2 (MCTR2) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages at the site of inflammation. DHA is oxidized to maresin 1 , which is converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase then to MCTR2 by γ-glutamyl transferase. MCTR2 accelerates tissue regeneration in planaria (1 and 100 nM). Pretreatment with MCTR2 prior to E. coli administration reduces neutrophil infiltration, shortens the inflammatory resolution period, and increases phagocytosis of E. coli by macrophages. When administered at a dose of 100 ng 12h post E. coli infection in a mouse model of peritonitis, MCTR2 selectively reduced the amount of the eicosanoids PGD2 and PGF2α in the exudate.

Maresin conjugates in tissue regeneration 3 (MCTR3) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages. DHA is oxidized to maresin 1 , which is converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase, then to MCTR2 by γ-glutamyl transferase, and to MCTR3 by dipeptidase. MCTR3 accelerates tissue regeneration in planaria (1 and 100 nM) approximately as potently as MCTR2 and more potently than MCTR1. Pretreatment with MCTR3 prior to E. coli administration in mice reduces neutrophil infiltration, shortens the inflammatory resolution period, and increases phagocytosis of E. coli by macrophages. When administered at a dose of 100 ng 12h post E. coli infection in a mouse model of peritonitis, MCTR3 selectively reduces the amount of the eicosanoids PGD2 , PGE2 , PGF2α , and TXB2 in the exudate.

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]