monocytes

Dexamethasone is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory, immunosuppressive, and apoptosis-inducing activities. It inhibits the production of inflammatory miRNA-155 exosomes in macrophages, significantly reduces inflammatory cytokine expression in neutrophils and monocytes, suppresses LPS-induced macrophage inflammation, and induces autophagy. It is commonly used to induce animal models of depression, muscle atrophy, and hypertension, and holds potential in COVID-19 research.

L-Leucyl-L-Leucine methyl ester hydrochloride (Leu-Leu-ome hydrochloride) is a dipeptide condensation product of L-leucine methyl ester produced by human monocytes or polymorphonuclear leukocytes. L-Leucyl-L-Leucine methyl ester hydrochloride selectively eliminates lymphocytes with cytotoxic potential and also induces lysosomal stress.

Phellopterin is a partial agonist of the central benzodiazepine receptors in vitro. Phellopterin shows a cytotoxic effect on RAW264.7 cell at the concentration from 40 to 400 μM. Phellopterin reduce TNF-alpha-induced VCAM-1 expression through regulation o

Adalimumab (anti-TNF-alpha) is the first fully human recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha.

LM-1685 is a potent and selective inhibitor of COX-2 IN human monocytes and whole blood with IC50 of 0.65µM and IC50 = 4.3μM, respectively, and is a potential compound for the treatment of inflammation.

IL-4 inhibitor is an inhibitor of IL-4.1It binds to IL-4 with a Kdvalue of 1.8 μM and inhibits IL-4 activity in a cell-based reporter assay (EC50= 1.81 μM). It is selective for IL-4 over IL-13 (EC50= 18.2 μM). IL-4 inhibitor inhibits IL-4-induced STAT6 phosphorylation in THP-1 monocytes (EC50= 3.1 μM), indicating inhibition of the IL-4-JAK1-STAT6 signaling pathway.

Indobufen (Ibustrin) is an inhibitor of platelet aggregation and is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes.

Geranylgeraniol (FT0626663) is an isoprenoid found in fruits, vegetables, and grains, including rice. Geranylgeraniol (FT0626663) inhibits growth and induces apoptosis of various tumor cells. Geranylgeraniol (FT0626663) protects monocytes against statin-induced cytotoxicity and suppresses the growth of Mycobacterium.

SKF-86002 is an effective inhibitor of p38 MAP kinase (IC50: 0.5-1 uM); inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50: 1 μM).

ACT-389949 is a potent and selective agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. It has the potential for the treatment of inflammatory disorders.

LR-90, an advanced glycation end product (AGE) inhibitor, is utilized in diabetic animal model research. This compound effectively suppresses inflammatory responses in human monocytes.

CCX140 (CCX140-B) (CCX140-B) is an antagonist of CCR2.

Lobucavir inhibits the replication of the HIV virus in T cells, monocytes & macrophages in vitro by inhibiting DNA polymerase and viral DNA synthesis.

IX-207-887 is an innovative anti-arthritis compound that effectively inhibits the release of interleukin-1 (IL-1) from human monocytes and murine peritoneal macrophages in vitro. Its active concentration can reach therapeutic levels in both human rheumatoid arthritis and animal arthritis models. Furthermore, IX-207-887 exhibits a novel ability to suppress IL-1 release.

Fosfenopril (Fosinoprilat) is a potent angiotensin-converting enzyme (ACE) inhibitor that mitigates lipopolysaccharide-induced inflammation in monocytes through the suppression of TLR4/NF-κB signaling pathways, and Fosfenopril is utilized in cardiovascular and anti-inflammatory research to investigate molecular mechanisms of ACE inhibition.

GHN105 is an orally active STING inhibitor that suppresses STING-dependent IFN-β secretion in THP-1 human monocytes with an IC50 of 4.4 μM. In mice, GHN105 reduces serum levels of IFN-β, IL-6, and CXCL10, and alleviates colitis in a DSS-induced acute colitis mouse model. Additionally, GHN105 demonstrates favorable pharmacokinetic properties in mice, with an oral bioavailability of 43% and a half-life of 1.1 hours.

NK7-902 is a CRBN molecular glue degrader of NEK7. It fully degrades NEK7 in human primary monocytes and whole blood, yet only partially inhibits NLRP3-dependent IL-1β production. NK7-902 results in profound and lasting degradation of NEK7, but only temporarily blocks NLRP3 inflammasome activation in non-human primates via oral administration. The compound demonstrates activity in mouse systems.

Aluminum phosphate adjuvant is a safe and effective adjuvant that activates the immune system and associated pathways in monocytes.

GPR183 antagonist-3 (compound 33) is an orally active GPR183 antagonist with an IC50 value of 8.7 μM. It demonstrates significant in vitro anti-migration and anti-inflammatory activity in monocytes and can alleviate pathological symptoms in experimental colitis induced by dextran sulfate sodium.

endo-S-cGAFMP (Compound 3) is a STING agonist that enhances both innate and adaptive immune responses by activating the cGAS-STING pathway, leading to the production of interferon regulatory factors and pro-inflammatory cytokines. It exhibits strong immunostimulatory activity in THP1 monocytes and RAW macrophages, with EC50 values of 2.45 μM and 5.54 μM, respectively. endo-S-cGAFMP also demonstrates significant antitumor activity and holds potential as an immunotherapy agent for cancer, particularly in studies involving systemic administration.

PROTACIRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader, demonstrating DC50 values of 0.86 nM and 1.1 nM in monocytes and lymphocytes within PBMCs, respectively. It significantly induces TIR signaling activation and inhibits the expression of circulating pro-inflammatory cytokines in a psoriasis mouse model induced by Imiquimod. PROTACIRAK4 degrader-13 is applicable in the study of neutrophilic inflammatory diseases driven by TLR and IL-1R, such as hidradenitis suppurativa (HS) and atopic dermatitis (AD).

NK7-902 TFA is a CRBN molecular glue degrader of NEK7. It effectively degrades NEK7 in human primary monocytes and whole blood, yet only partially inhibits NLRP3-dependent IL-1β production. While NK7-902 TFA achieves deep and lasting NEK7 degradation, it temporarily blocks NLRP3 inflammasome activation in non-human primates when administered orally. Additionally, NK7-902 TFA demonstrates activity in mouse systems.

TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (with a lowest effective concentration (LEC) [hTLR7] of 1.6 μM) and TLR8 (LEC [hTLR8] of 1.6 μM). It acts on human peripheral blood mononuclear cells (hPBMC) with agonistic activity (LEC [hPBMC] = 0.5 μM). In mice and cynomolgus monkeys, TLR7/8 agonist 13 induces endogenous IFNα, activates myeloid dendritic cells and monocytes, promoting their differentiation towards a TH1 phenotype. In chronic AAV-HBV mouse models, it reduces viral load and HBV surface antigen levels. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, facilitating the response of HBV antigen-specific CD8 T cells. This compound is useful for hepatitis B virus research.

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.