Astragaloside VI could activate EGFR/ERK signalling pathway to improve wound healing.
HI-236 is used as a non-nucleoside HIV-1 reverse-transcriptase inhibitor.
Acetaminophen (paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic drug.
Gardenin A is an orally active and synthetic PMF analogue with the neurotrophic effect for neurite outgrowth and neuronal differentiation. Gardenin A promotes neuritogenesis via activating MAPK/ERK, PKC, and PKA, but not TrkA, CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects[1][2].
α-Humulene is a main constituent of Tanacetum vulgare L. (Asteraceae) essential oil with anti-inflammation (IC50=15±2 µg/mL). α-Humulene inhibits COX-2 and iNOS expression[1].
RORγ-IN-1 is a RORγ inhibitor extracted from patent US 9481674 B1, has a Ki of <100 nM.
5,6,7-Trimethoxyflavone is a novel p38-α MAPK inhibitor with an anti-inflammatory effect. 5,6,7-Trimethoxyflavone is isolated from several plants including Zeyhera tuberculosa, Callicarpa japonica, and Kickxia lanigera[1].
Chlorpheniramine maleate is an histamine H1 receptor antagonist with IC50 of 12 nM.Target: Histamine H1 ReceptorChlorpheniramine inhibits the proliferation of MCF-7, MDA-MB 231, and Ehrlich cells in a dose-response manner, and significantly reduces the ornithine decarboxylase mRNA translation by 50%-70% at the 250 μM [1]. Chlorpheniramine displaces of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells with IC50 of 66 nM. Chlorpheniramine displays antimalarial activity against CQS strain (D6) and MDR strain (Dd2) of P. falciparum with IC50 of 61.2 uM and 3.9 uM, respectively. Chlorpheniramine displays cytotoxicity against the proliferation of concanavalin A-induced murine splenic lymphocytes with IC50 of 33.4 μM [2].Oral administration of Chlorpheniramine inhibits histamine-induced mortality in guinea pigs with an ED50 of 0.17 mg/kg [3]. Oral administration of Chlorpheniramine (10 mg/kg) significantly inhibits short-duration scratching in BALB/c mice stimulated by ovalbumin active cutaneous anaphylaxis and in ICR mice subcutaneously injected with histamine, but not long-duration scratching seen in NC/Nga mice, in contrast to that of dexamethasone or tacrolimus [4].
4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever[1][2][3]. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties[2].
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM[1]. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity[2].
MK-571-d6 (L-660711-d6) sodium salt is the deuterium labeled MK-571 sodium salt. MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist, with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes[1][2].
Flosulide is a potent and selective COX-2 inhibitor, used for the treatment for inflammatory diseases.
HadAB-IN-1 is a potent HadAB inhibitor. HadAB-IN-1 inhibits HadAB enzyme complexes activity with an IC50 value of 0.03 μM. HadAB-IN-1 also affects mycolic acid biosynthesis in Mycobacterium tuberculosis (Mtb). HadAB-IN-1 can be used for the research of tuberculosis (TB)[1].
Orticumab (MLDL1278A) is an antibody targeting to oxidized or malondialdehyde-modified lipoprotein (LDL). Orticumab specifically inhibits oxidized low-density lipoproteins (oxLDL). Orticumab involves in modulation of autoimmune responses against oxLDL, improves atherosclerosis in animal model. Orticumab also can be used for research of psoriasis improvement[1][2].
BC-1471 is a STAM-binding protein (STAMBP) deubiquitinase inhibitor. BC-1471 inhibits NALP7 (NACHT, LRR and PYD domains-containing protein 7) inflammasome activity[1].
ROCK2-IN-6 (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research[1].
(+)-Borneol (d-Borneol) is a natural bicyclic monoterpene used for analgesia and anesthesia in traditional Chinese medicine; enhances GABA receptor activity with an EC50 of 248 μM.
Beta-asarone is a major ingredient of Acorus tatarinowii Schott, penetrates blood brain barrier, with the properties ofimmunosuppression, central nervous system inhibition, sedation, and hypothermy. Beta-asarone protects against Parkinson’s disease[1].
Glucametacine is an anti-inflammatory agent[1].
Columbianadin, a natural coumarin from, is known to have various biological activities including anti-inflammatory and anti-cancer effects.
ODN 2216 is a TLR9 (toll-like receptor 9) ligand or agonist. ODN 2216 induces high amounts of IFN-α and IFN-β. ODN 2216 induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 can activate NK cells and promote IFN-γ production of TCR-triggered CD4+ T cells[1][2][3][4].
Isorhamnetin 3-O-galactoside (Cacticin), a flavonoid glycoside isolated from Artemisia capillaris Thunberg, which ameliorates CCl4-induced hepatic damage by enhancing the anti-oxidative defense system and reducing the inflammatory signaling pathways. Isorhamnetin 3-O-galactoside (Cacticin) has antithrombotic and anti-inflammatory activities[1][2][3].
ADU-S100 is an inducer of STING (stimulator of interferon genes). ADU-S100 has enhanced binding affinity to STING and activate all known human STING alleles.
Quinotolast sodium in the concentration range of 1-100 μg/mL inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner.
Sibiricine (Compound 8) is an isoquinoline alkaloid derived from the medicinal plant Corydalis crispa. Sibiricine has significant anti-inflammatory activity on TNF-α production by LPS-activated THP-1 cells[1].
Gimsilumab (MORAb-022) is a humanized anti-GM-CSF monoclonal antibody. Gimsilumab has the potential for the research of COVID-19 and rheumatoid arthritis (RA)[1][2].
Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity[1].
1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid is from Cordyceps bassiana, which is one of Cordyceps species with anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity, anti-angiogenic, and anti-nociceptive activities. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid targets to block AP-1-mediated luciferase activity, implying it has an anti-inflammatory function[1].
Colcemid (Demecolcine), a derivative of colchicine, is a potent mitotic inhibitor[1][2]. Colcemid binds to the protein tubulin and arrest cells in metaphase for karyotyping assays. Colcemid incuces cell apoptosis and can be used for cancer research[2].
Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 microM), while not affecting ADP- or arachidonic acid-induced platelet aggregation [1]. The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7+/-0.4 microM, 3.2+/-0.7 microM and 1.5+/-0.4 microM, respectively whereas for loratadine the IC50 was 2.1+/-0.9 microM, 4.0+/-1.3 M and 1.7+/-0.5 microM. SR-27417A exhibited no inhibitory effect [2].in vivo: Rupatadine blocked histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 micrograms/kg i.v.). Moreover, it potently inhibited PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg/kg i.v.) [1]. rupatadine treatment improved the declined lung function and significantly decreased animal death. Moreover, rupatadine was able not only to attenuate silica-induced silicosis but also to produce a superior therapeutic efficacy compared to pirfenidone, histamine H1 antagonist loratadine, or PAF antagonist CV-3988 [3].