C8 Galactosylceramide is a synthetic C8 short-chain derivative of known membrane microdomain-forming sphingolipids. It increases the amount delivered and toxicity of doxorubicin in cancerous but not non-cancerous cells when incorporated into the nanoliposomal membrane of nanoliposomal-doxorubicin. C8 Galactosylceramide induces proliferation and cytokine production by splenocytes in vitro at concentrations ranging from 100-1,000 ng/ml but has no effect on natural killer T cell production in vivo. It also activates NF-κB production in C6 glioma cells when used at a concentration of 10 μM.

Sulfatides are endogenous sulfoglycolipids with various biological activities in the central and peripheral nervous systems, pancreas, and immune system. They are produced from the combination of ceramide and UDP-galactose in the endoplasmic reticulum followed by sulfation in the Golgi apparatus. The ceramide portion contains variable fatty acid chain lengths, which are tissue- and pathology-dependent. Sulfatides are primarily found in the myelin sheath of oligodendrocytes and Schwann cells, with smaller chain lengths predominant during development and longer chain lengths predominant in mature cells. They accumulate in the lysosome of patients with metachromatic leukodystrophy, a disorder characterized by arylsulfatase A deficiency. Sulfatides are also located in pancreatic β-cells and inhibit insulin release from isolated rat pancreatic islet cells, suggesting a potential role in diabetes. Sulfatides can induce inflammation in glia in vitro and certain sulfatides, such as C24:1 3'-sulfo-galactosylceramide, can induce an immune response in vitro in mouse splenocytes. Sulfatides (bovine) (sodium salt) is a mixture of isolated bovine sulfatides.

Risankizumab (BI 655066) is a humanized IgG monoclonal antibody (Kd <10 pM) targeting the IL-23 p19 subunit. Risankizumab inhibits IL-17 production induced by human IL-23 in mouse splenocytes with an IC50 value of 2 pM.Risankizumab is used for the prevention and treatment of immune and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis, and erythrodermic psoriasis.

α-Galactosylceramide analog 8 (α-GalCer analog 8) is a triazole derivative of α-galactosylceramide. [1] It increases IL-2 secretion by DN32.D3 NKT hybridoma cells when co-cultured with CD1d-transfected RBL cells pre-loaded with α-GalCer analog 8 at a concentration of 32 ng/ml. α-GalCer analog 8 (32 ng/ml) induces IL-4 secretion to a greater extent than the synthetic α-GalCer KRN 7000 in mouse splenocytes in vitro and in mouse serum following administration of a 1 µg per animal dose, indicating a Th2 response.

Tetracosanoyl-sulfatide is an endogenous sulfated glycolipid, which are also known as sulfatides . Tetracosanoyl-sulfatide is the major sulfatide in mature myelin in the central and peripheral nervous systems. Levels of Tetracosanoyl-sulfatide are elevated in plasma derived from patients with metachromatic leukodystrophy, a disorder characterized by arylsulfatase A deficiency, leading to sulfatide accumulation. Unlike C24:1 3'-sulfo galactosylceramide, it does not induce an immune response in mouse splenocytes in vitro.

Peficitinib (ASP015K) (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.

Carviolin is an anthraquinone fungal metabolite that has been found inZ. longicaudatawith immunosuppressive and antitrypanosomal activities.1,2It inhibits LPS- or concanavalin A-induced proliferation of mouse splenocytes (IC50s = 4 and 4.5 μg/ml, respectively).1Carviolin is active againstT. b. brucei(MIC = 41.66 μM).2 1.Fujimoto, H., Nakamura, E., Okuyama, E., et al.Six immunosuppressive features from an ascomycete, Zopfiella longicaudata, found in a screening study monitored by immunomodulatory activityChem. Pharm. Bull. (Tokyo)52(8)1005-1008(2004) 2.Aly, A.H., Debbab, A., Clements, C.M., et al.NF kappa B inhibitors and antitrypanosomal metabolites from endophytic fungus Penicillium sp. isolated from Limonium tubiflorumBioorg. Med. Chem.19(1)414-421(2011)

(-)-Rasfonin is a fungal metabolite that has been found in T. terrophilus.1 It inhibits proliferation of mouse splenocytes induced by concanavalin A and LPS (IC50s = 0.7 and 0.5 μg/ml, respectively). References1. Fujimoto, H., Okamoto, Y., Sone, E., et al. Eleven new 2-pyrones from a fungi imperfecti, Trichurus terrophilus, found in a screening study guided by immunomodulatory activity. Chem. Pharm. Bull. (Tokyo) 53(8), 923-929 (2005).

C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z)) is the predominant sulfate analog in the mature myelin sheath. C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z)) interacted with C-type lectin and immunoglobulin-like receptors to give the highest affinity for LMIR5. Galactosylceramide (d18:1/24:1(15Z)) induces MCP-1 production by basophils, which activates NFAT by increasing LMIR5, but not mast cells .C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z)) binds in vitro to CD1d binding and increased the proliferation of free mouse splenocytes.

Maydispenoid B, a potent immunosuppressor, effectively inhibits the proliferation of murine splenocytes activated by anti-CD3/anti-CD28 monoclonal antibodies (mAbs) and lipopolysaccharide.

Rosiptor is a potent and selective SHIP1 activator. AQX-1125 inhibits Akt phosphorylation in SHIP1-proficient but not in SHIP1-deficient cells, reduces cytokine production in splenocytes, inhibits the activation of mast cells and inhibits human leukocyte

ML604440 is a cell permeable proteasome β1i (LMP2) subunit inhibitor.

Ganoderic acid LM2 exhibits potent enhancement of ConA-induced mice splenocytes proliferation in vitro.

1. Geraniin has a protective effect against OVX-induced rat osteoporosis. 2. Geraniin has cytotoxic activity towards cancer cells in vitro and in vivo. 3. Geraniin exerts inhibitory effects on osteoclast differentiation in vitro and suppresses Ti particle

Colletodiol is a fungal metabolite that has been found inD. grovesiiand has immunosuppressant and antiviral activities.1,2It inhibits concanavalin A- or LPS-induced proliferation of isolated mouse splenocytes (IC50s = 12 and 5 μg/ml, respectively).1Colletodiol inhibits influenza A viral replication in HeLa-IAV-Luc cells.2 1.Fujimoto, H., Nagano, J., Yamaguchi, K., et al.Immunosuppressive components from an ascomycete, Diplogelasinospora grovesiChem. Pharm. Bull.46(3)423-429(1998) 2.Lai, W., Wang, S., and Ye, X.Colletodiol inhibits the replication of influenza A virus WSN/H1N1 by reducing the activity of viral RNA polymeraseWei Sheng Wu Xue Bao53(12)1334-1339(2013)

KBC-007 is a synthetic branched chain-containing analog of α-galactosylceramide (α-GalCer). It induces IL-4 and IFN-γ secretion by mouse splenocytes when used at a concentration of 0.5 ng/ml and IL-2 secretion by DN32.D3 NKT hybridoma cells co-cultured with CD1d-transfected RBL cells pre-loaded with KBC-007 at a concentration of 8 ng/ml. KBC-007 (1 μg per animal) increases levels of IL-4, but not IFN-γ, to a similar degree as α-GalCer in mouse serum. KBC-007 (0.5 μg per animal) increases the survival rate of mice immunized with the inactivated influenza A virus A/PR/8/34 in a model of influenza infection.

Tetrachlorohydroquinone (TCHQ) is a metabolite of the organochlorine biocide pentachlorophenol. It is cytotoxic to RTL-W1 rainbow trout liver cells (EC50 = 1.55 μM in a neutral red assay). TCHQ increases production of reactive oxygen species (ROS), inhibits apoptosis, and induces loss of the mitochondrial membrane potential and necrosis in splenocytes. In vivo, TCHQ induces glutathione (GSH) depletion in mouse liver.

Kaempferitrin (Lespenephryl) has antidepressant-like effect related to the serotonergic system, principally 5-HT1A. Kaempferitrin exerts cytotoxic and antitumor effects against HeLa cells. Kaempferitrin stimulates glucose-metabolizing enzymes, promotes glucose homeostasis. Kaempferitrin exerts immunostimulatory effects on immune responses mediated by splenocytes, macrophages, PBMC and NK cells. Kaempferitrin induces cytotoxic effects to include: cell cycle arrest in G1 phase and apoptosis via the intrinsic pathway in a caspase-dependent pathway.

Mianserin, an H1 receptor reverse agonist, is a psychoactive compound in the tetracyclic antidepressant (TeCA) treatment family. Mianserin has antidepressant, antianxiety, antiemetic, hypotrophic, hypnotic and antihistamine effects, and can be used as a combination of norepinephrine and specific serotonin to treat depression.