immune-modulating

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).

Laminaran is a β-1,3-glucan isolated from brown algae, often serving as a typical ligand for Dectin-1. It possesses anti-cancer, immune-modulating, and radiation-protective properties. Laminaran can be catalyzed by glucanase. In in vitro and in vivo experiments, Laminaran has demonstrated anti-tumor activity and may be used for severe cancers.

Fucoidan is found in various species of brown seaweed and algae,with anticancer, antiviral, neuroprotective, immune-modulating.

FCE-27164 is a therapeutic agent that inhibits the binding of platelet-derived growth factor beta and interleukin-7 (IL-7) to their respective receptors, potentially modulating inflammatory and immune responses.

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.

MS40 is a WDR5 PROTAC that selectively degrades WDR5 and serves as a novel degrader for immune-modulating compounds (IMiDs), including the new substrates CRBN and Ikaros zinc finger (IKZF) transcription factors IKZF1 and IKZF3. MS40 facilitates the degradation of WDR5, resulting in the dissociation of the MLL/KMT2A complex from chromatin, thereby reducing H3K4me2 levels. In vitro, MS40 inhibits the growth of primary leukemia patient cells, and in vivo, it suppresses the expansion of patient-derived xenografts.

ZM522 is a CD73 inhibitor with an IC50 value of 0.56 μM. It effectively increases interferon-gamma (INF-γ) levels and enhances immune activity by modulating T cell activation. ZM522 holds potential for research in immunology and anti-cancer fields.

Cbl-b-IN-28 (Compound B2) is an orally active Cbl-b inhibitor. It enhances the function of immune cells by promoting the secretion of cytokines like IL-2 and modulating the phosphorylation levels of key proteins in the T cell receptor signaling pathway. Cbl-b-IN-28 is applicable in cancer immunology research.

FPPS-IN-11 is a potent inhibitor of farnesyl pyrophosphate synthase (FPPS) that effectively blocks a key enzymatic step in the mevalonate pathway, thereby modulating downstream isoprenoid biosynthesis, protein prenylation processes, and cholesterol-associated signaling pathways that are critically involved in cell proliferation, immune regulation, and metabolic disease progression.

Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic double-stranded RNA (dsRNA) analog and an agonist of TLR3 as well as retinoic acid-inducible gene I (RIG-I) and melanoma differentiation-associated protein 5 (MDA5). It can induce innate immune responses in mammals and serve as a vaccine adjuvant to enhance both innate and adaptive immunity, while modulating the tumor microenvironment and directly inducing apoptosis in cancer cells. Poly(I:C) is commonly used to establish acute respiratory distress syndrome (ARDS) animal models for studying immune responses and disease mechanisms.

AIM-102, a nonsteroidal, immune modulating, anti-inflammatory drug, is used potentially for the treatment of allergic asthma.

Norcholic Acid (Nor Cholic Acid) is a bile acid that promotes tumor progression and immune escape by modulating the farnesol X receptor in hepatocellular carcinoma.Norcholic Acid is efficiently absorbed from the intestine and is rapidly secreted into the bile.

Potent inhibitor of NF-κB activation (IC50 = 85 nM); decreases IκBα phosphorylation. Attenuates LPS-induced nitric oxide production and expression of TNF-α, IL-6 and MCP. Suppresses proliferation of HeLa and HCT116 cells. Anti-inflammatory and antitumor. Hu et al (2007) Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases. Chem.Biol. 14 764 PMID:17656313 |Johnson et al (2012) Myxobacteria versus sponge-derived alkaloids: the bengamide family identified as potent immune modulating agents by scrutiny of LC-MS/ELSD libraries. Bioorg.Med.Chem. 20 4348 PMID:22705020 |Kinder et al (2001) Synthesis and antitumor activity of ester-modified analogues of bengamide B. J.Med.Chem. 44 3692 PMID:11606134

1. Cucurbitacin IIb is one of the major active compounds in Hemsleyadine tablets which have been used for clinical treatment of bacillary dysentery, enteritis and acute tonsilitis. 2. Cucurbitacin IIb exhibits its anti-inflammatory activity through modula

Soyacerebroside II exhibits ionophoretic activity for Ca2+ ion. Soyacerebrosides I and II have modulating the cellular immune response effects, they show obvious inhibitory activity on IL-18 secretion in human peripheral blood mononuclear cells (PBMC).

KM04416 is a GPD2 inhibitor that inhibits LUAD progression by modulating immune cell infiltration.

L-Inosine, the L-configuration of Inosine, is an endogenous purine nucleoside derived from adenosine catabolism. It exhibits anti-inflammatory, antinociceptive (pain-relieving), immunomodulatory (immune system-modulating), and neuroprotective effects [1] [2].

Fidasimtamab is a recombinant human IgG1 bispecific antibody designed to target and inhibit both HER2 and PD-1 signaling pathways. Fidasimtamab bridges PD-1 expressing T cells with HER2 expressing tumor cells, thereby modulating immune responses while exhibiting potential immunosuppressive and antitumor effects. This mechanism provides an unique therapeutic approach for cancer research.

Mirikizumab (LY3074828) is a humanized monoclonal antibody targeting the p19 subunit of interleukin-23 (IL-23), modulating immune response by inhibiting IL-23 binding to IL-23R, used in studies of ulcerative colitis.

HCV-1 e2 Protein (554-569) TFA, an antigenic segment of the hepatitis C virus envelope 2 (e2) protein, contains a potential N-glycosylation site that may influence immune recognition of e2 [1].

Ziralimumab (ABX-RB2) is a monoclonal antibody that targets and inhibits IL-2 receptor, thereby modulating the immune response.

Spns2-IN-1 is a potent Spns2 inhibitor, effectively impeding Spns2-dependent S1P transport with an IC50 value of 1.4±0.3 μM, crucial for modulating the immune response [1].

Erzotabart is an IgG1-kappa monoclonal antibody that targets human CD38 (also known as ADP-ribosyl cyclase 1 or cyclic ADP-ribose hydrolase 1) and displays pronounced antineoplastic activity. Erzotabart acts by modulating CD38-mediated signaling pathways involved in tumor cell metabolism, proliferation, and immune evasion, making it a significant investigational candidate in oncology research.