MLN3126 (MLN 3126, MLN-3126) is a potent, selective, orally available CCR9 antagonist with IC50 of 6.3 nM (CCL25-induced calcium mobilization); shows no significant antagonistic activity for other 12 chemokine receptors (CCR1, -2b, -4, -6, -7, -8, -10,CX3CR1, CXCR1, -2, -3 and -4) at 10 uM; dose dependently inhibits CCL25-induced chemotaxis of mouse thymocytes (IC90=1.8 uM); ameliorates inflammation in a T cell mediated mouse colitis model. Other Indication Phase 1 Discontinued
Sulfo-SPDB linker is a disulfide-cleavable linker used for the antibody-drug conjugate (ADC)[1].
Thunalbene is a stilbene derivative isolated from Thunia alba. Thunalbene has a weak inhibitory effect on nitric oxide production and is not cytotoxic[1].
Herpotrichone B shows potent anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) value of 0.11 μM.
Limonene is a monoterpene in citrus peel oil. A popular disinfectant and food preservative. Antimicrobial activities[1]. Anti-proliferative activities[2]. Antioxidant and anti-inflammatory effect[3].
Alintegimod (7HP349) is a potent and orally active integrin activator. Alintegimod can serve as a systemically administered adjuvant to enhance T cell-mediated immune responses to vaccines[1].
CDN-A is a cyclic di-nucleotide, it can be used to synthesis antibody-drug conjugate (ADC). Cyclic di-nucleotides are potent stimulators of innate and adaptive immune responses. In humans, cyclic di-nucleotide, which are either produced endogenously in response to foreign DNA or by invading bacterial pathogens, trigger the innate immune system by activating the expression of interferon genes[1][2][3].
AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.
GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury[1][2][3].
Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.
Methyl nicotinate, the methyl ester of Niacin found in alcoholic beverages, that is used as an active ingredient as a rubefacient in over-the-counter topical preparations indicated for muscle and joint pain[1].
Mulberrofuran H is a 2-arylbenzofuran derivative from the cultivated mulberry tree (Morus lhou (ser.) Koidz.). Mulberrofuran H demonstrates potent inhibition against substrates L-tyrosine (IC50=4.45 µM) and L-DOPA (IC50=19.70 µM). Mulberrofuran H also shows potent anti-inflammatory and antioxidative activities[1][2][3].
SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid[1][2][3].
Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].
Benzylurea is a benzylamide. Benzylurea can be isolated from Salvadora persica stems. Benzylurea has antimicrobial activity. Benzylurea can be used for the research of various biochemical studies[1].
Oxidized ATP (oATP) trisodium salt is a broad-spectrum P2 receptor inhibitor. Oxidized ATP trisodium salt irreversibly antagonizes P2X7R activation. Oxidized ATP trisodium salt inhibits c-reactive protein (CRP)-induced NLRP3 inflammasome activation. Oxidized ATP trisodium salt can be used for research of atherosclerosis[1][2].
Benzoylgomisin P is an anti-inflammatory agent[1].
PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively[1].
Antcin A is a potent NLRP3 inhibitor that inhibits the assembly and activation of the NLRP3 inflammasome. Antcin A can inhibit Kupffer cell pyroptosis and has liver protective activity. Antcin A can be used to study inflammation, such as non-alcoholic fatty liver disease[1].
MALT1-IN-11 (Example 151 in reference Patent) is a MALT1 protease inhibitor (IC50 < 10 nM). MALT1-IN-11 inhibits IL10 secretion with an IC50 of 10-100 nM. MALT1-IN-11 can be used for the research of cancer, autoimmune and inflammatory disorders[1].
DT-3 is a membrane-permeable protein kinase G Iα inhibitory peptide. DT-3 is a guanylyl cyclase? inhibitor and shows pharmacological blockade of the cGMP–PKG signalling[1].
Glucocorticoid receptor agonist-1-Gly-Gly-Glu-Gly-Br is a steroid-Linker conjugate used for the synthesis of immunoconjugates linked to proteins[1].
Gingerenone A is a Nrf2-Gpx4 activator with anti-breast-cancer properties. Gingerenone A results a delayed G2/M in cancer cells, following oxidative stress and senescence responses. Gingerenone A also alleviates ferroptosis in secondary liver injury (SLI) in dextran sodium sulfate (DSS)-induced colitis mice. Gingerenone A can be isolated from Zingiber officinale[1][2].
(+)-(3R,8S)-Falcarindiol is a polyacetylene found in carrots, has antimycobacterial activity, with an IC50 of 6 μM and MIC of 24 μM against Mycobacterium tuberculosis H37Ra[1][2]. Antineoplastic and anti-inflammatory activity[2].
Uralsaponin D is a saponin that can be isolated from Glycyrrhiza inflata. Uralsaponin D inhibits phospholipase A2 (PLA2) with an IC50 value of 32.2 μM[1].
Galicaftor (ABBV-2222; GLPG-2222) is a potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. Galicaftor can be used for cystic fibrosis research[1].
Atibuclimab, is a chimeric monoclonal antibody directed against CD14 and is composed of murine variable and human IgG4 Fc regions. Atibuclimab can be used for the research of amyotrophic lateral sclerosis[1]. Atibuclimab attenuates LPS-induced symptoms and strongly inhibits LPS-induced proinflammatory cytokine release, while only delaying the release of the anti-inflammatory cytokines soluble TNF receptor type I and IL-1 receptor antagonist[2].
Arachidonic acid is an essential fatty acid and a major constituent of biomembranes.
SIRT5 Inhibitor 6 is a potent, substrate-competitive and selective SIRT5 inhibitor with an IC50 of 3.0 μM. SIRT5 Inhibitor6 has a therapeutic potential against septic AKI in vivo[1].
Tavilermide is a selective, partial agonist of TrkA, or a nerve growth factor (NGF) mimetic.