dendritic

Immethridine dihydrobromide is a novel, highly potent and selective histamine H3 receptor (H3R) agonist that inhibits dendritic cell function and alleviates experimental autoimmune encephalomyelitis.Immethridine dihydrobromide MesV induces depolarization of neurons and the MMN and prevents cardiorenal and renal injury. injury.

GGTI 2147 FA, a selective GGT inhibitor, abolishes bicuculline-induced increase in dendritic spine density in hippocampal experiments and may reduce learning and memory abilities in mice.

GSK-J4 (GSK J4 HCl) is a cell permeable prodrug of GSK-J1, a dual inhibitor of the H3K27me3 me2 demethylases JMJD3 KDM6B and UTX KDM6A (IC50=8.6 6.6 μM). GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

3-Hydroxykynurenamine, also known as 3-Hydroxy-L-kynurenamine or 3-HKA, is a biogenic amine produced via an alternative pathway of tryptophan metabolism. In vitro, 3-HKA has an anti-inflammatory profile by inhibiting the IFN-γ mediated STAT1 NF-κΒ pathway in both mouse and human dendritic cells (DCs) with a consequent decrease in the release of pro-inflammatory chemokines and cytokines, most notably TNF, IL-6, and IL12p70. 3-HKA has protective effects in an experimental mouse model of psoriasis by decreasing skin thickness, erythema, scaling and fissuring, reducing TNF, IL-1β, IFN-γ, and IL-17 production, and inhibiting generation of effector CD8+ T cells. Similarly, in a mouse model of nephrotoxic nephritis, besides reducing inflammatory cytokines, 3-HKA improves proteinuria and serum urea nitrogen, overall ameliorating immune-mediated glomerulonephritis and renal dysfunction.This compound is unstable in powder form and other related salt forms are recommended.

G0-C14 HCl is the salt form of G0-C14, a cationic lipid molecule and amphiphilic dendritic macromolecule commonly used in the synthesis of nanoparticles and vaccine delivery.

Jagged-1 (188-204)is a fragment of the JAG-1 protein. JAG-1 is Notch ligand, a peptide that is the most conspicuously expressed ligand in skin. JAG-1 induces epidermal maturation. Exposing submerged keratinocytes monolayers to JAG-1 with elevated calcium concentration produces stratification with loricrin expression and NF-αB activation.

ADH-503 (GB1275) is an orally available, allosteric CD11b small molecule agonist that can lead to repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhancement of dendritic cell responses.

(Z)-Leukadherin-1 (ADH-503 free base) is an allosteric agonist of CD11b.

7α,25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist, as well as an endogenous ligand, of the orphan GPCR receptor EBI2 (GPR183). It serves as a chemokine directing the migration of B cells, T cells, and dendritic cells and exhibits high potency in activating EBI2 (EC50=140 pM; Kd=450 pM) [1][2].

Resolvin E1 is an effective endogenous pro-resolving mediator of inflammation. Resolvin E1 has unique counterregulatory actions that inhibit PMN transendothelial migration. Resolvin E1 also acts as an effective inhibitor of leukocyte infiltration, dendrit

1Z105, an orally active TLR4 MD2 ligand, facilitates dendritic cell maturation and antigen presentation, thereby preventing arthritis.

NOD2 agonist 2 (compound 23) enhances antigen presentation in murine bone marrow-derived dendritic cells (BMDCs), highlighting its potential as a vaccine adjuvant.

Perfluoroenanthic acid (Perfluoroheptanoic acid) is a perfluoroalkyl substance (PFAS) that negatively impacts spermatogenic development and testicular m6A RNA methylation in offspring exposed during gestation, thus impeding spermatogenesis and inducing reproductive toxicity. Additionally, in primary cortical neuron cultures, Perfluoroenanthic acid alters dendritic spine morphology and synaptogenesis, enhances neural activity and synaptic transmission, and increases the expression of excitatory synapse-associated proteins Synaptophysin and PSD95.

Apilimod (STA 5326) inhibits the production of IL-12 and IL-23 and reduces dendritic cell infiltration in psoriasis.

Lipid N2-3L is an ionizable cationic lipid with a pKa of 8.99, utilized in the formation of supramolecular lipid nanoparticles (SMLNPs) for enclosing mRNA in both in vitro and in vivo applications. Lipid N2-3L-containing SMLNPs accumulate at the injection site and draining lymph nodes in mice, featuring a luciferase reporter gene. Additionally, SMLNPs made with Lipid N2-3L that encapsulate ovalbumin mRNA and the Toll-like receptor 7 8 (TLR7 8) agonist R-848 serve as adjuvants. These enhance dendritic cell maturation and antigen presentation, reducing tumor volume and increasing survival rates in MC-38-OVA colon cancer mouse models.

Calcium influx inducer compound 634 is an agent that stimulates calcium entry. At a concentration of 10 µM, it can enhance the release of extracellular vesicles (EVs) from mouse bone marrow-derived dendritic cells (mBMDCs). Furthermore, Calcium influx inducer compound 634 (10 µM) increases the levels of surface CD86 and CD80 on mBMDCs, an effect that can be blocked by the calcium release-activated calcium channel inhibitor YM-58483.

9-Methyl-β-carboline is a cognitive enhancer with neuroprotective, neurorestorative, and anti-inflammatory properties. Its behavioral effects may be linked to hippocampal dopamine levels and the stimulation of dendritic and synaptic proliferation.

ISM012-042 is an orally active inhibitor of PHD1 and PHD2, with IC50 values of 1.9 and 2.5 nM, respectively. At a concentration of 2.5 μM, ISM012-042 protects Caco-2 cells from DSS-induced barrier damage. Additionally, in LPS-induced bone marrow-derived dendritic cells (BMDC) from mice, ISM012-042 exhibits anti-inflammatory properties by dose-dependently reducing the expression of IL-12 subunit IL-12p35 and TNF. It also restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 is useful for studying intestinal mucosal repair and immune disorders.

BIT225 is a human immunodeficiency virus type 1 Vpu inhibitor with antiviral activity that inhibits HIV-1 replication in bone marrow dendritic cells and inhibits ion channels formed by HIV-1 Vpu.

CM-414 is a dual inhibitor of HDACs and PDE5 for the Treatment of Alzheimer's Disease (IC50 values of 60 nM, 310 nM, 490 nM, 322 nM, and 91 nM against PDE5, HDAC1, HDAC2, HDAC3, and HDAC6, respectively). Chronic treatment of Tg2576 mice with CM-414 dimini

DG026 is a IRAP inhibitor. DG026 ables to selectively downregulate IRAP-dependent cross-presentation by dendritic cells but leave ERAP1-dependent cross-presentation unaffected.

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

1-Arachidonoyl lysophosphatidic acid is a phospholipid containing arachidonic acid at the sn-1 position. It has been found in rat brain as 37% of the arachidonic acid-containing lysophosphatidic acid (LPA) species and is a precursor to 1-arachidonoyl glycerol . 1-Arachidonoyl lysophosphatidic acid binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM. It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS. It also decreases differentiation of HT-29 human colon carcinoma cells to goblet cells in the presence of sodium butyrate.

NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively, in Gen2.2 cells in a concentration-dependent manner.2NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner.3It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12Dmouse orthotopic model of colorectal cancer. 1.Tan, L., Nomanbhoy, T., Gurbani, D., et al.Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2)J. Med. Chem.58(1)183-196(2015) 2.Pauls, E., Shpiro, N., Peggie, M., et al.Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cellsJ. Biol. Chem. 287(23)19216-19228(2012) 3.Ma, Q., Gu, L., Liao, S., et al.NG25, a novel inhibitor of TAK1, suppresses KRAS-mutant colorectal cancer growth in vitro and in vivoApoptosis24(1-2)83-94(2019)