Piriprost (U-60,257B) potassium is an inhibitor of leukotriene synthesis. Piriprost potassium inhibits the release of both leukotriene and histamine with an IC50 of 0.11 μM from isolated porcine lung cells. Piriprost potassium increases alkaline phosphatase (ALP) activity in cultured endometrial stromal cells[1][2].
ATB-346 is a novel hydrogen sulphide-releasing derivative of naproxen with markedly reduced toxicity.IC50 value:Target: COX-2 ATB-346 suppressed gastric prostaglandin E(2) synthesis as effectively as naproxen, but produced negligible damage in the stomach and intestine, Unlike naproxen and celecoxib, ATB-346 accelerated healing of pre-existing gastric ulcers. In a mouse airpouch model, ATB-346 suppressed cyclooxygenase-2 activity and inhibited leukocyte infiltration more effectively than naproxen. ATB-346 was as effective as naproxen in adjuvant-induced arthritis in rats, with a more rapid onset of activity. Unlike naproxen, ATB-346 did not elevate blood pressure in hypertensive rats [1]. Treatement with ATB-346 exhibited a significantly more rapid and sustained recovery of motor function, achieving greater than double the increase in locomotion score of the naproxen group by the 10th day of treatment. ATB-346 also significantly reduced the severity of inflammation (proinflammatory cytokines, apoptosis of neural tissue, and nitrosative stress) that characterized the secondary effects of SCI [2].
UCB-6876 is a novel inhibitor of TNF signalling by stabilising an asymmetric form of the trimer, displaying a concentration-dependent response curve and selectivity over the TNFR1 extracellular domain and control proteins.
1,6-Dihydro-4,7-epoxy-1-methoxy-3,4-methylenedioxy-6-oxo-3,8-lignan, a lignan derivative from the ethyl acetate soluble fraction of twigs of Magnolia denudate (Magnoliaceae), exhibits anti-platelet-activating factor (PAF) activity. PAF is a potent lipid mediator in inflammation and asthma[1].
Pelargonidin 3,5-diglucoside (chloride) is a natural pigment abundantly present in red fruits and vegetables. Pelargonidin 3,5-diglucoside (chloride) acts as a scavenger for reactive oxygen species and reactive nitrogen species . Pelargonidin 3,5-diglucoside (chloride) demonstrates inhibitory effects on enzymes involved in the production of ROS, RNS, and pro-inflammatory cytokines[1].
Ocrelizumab is an anti-CD20 antibody that depletes circulating immature and mature B cells but spares CD20-negative plasma cells. The effector mechanisms of Ocrelizumab are complement-dependent cytotoxicity and antibody-dependent cellular cytotoxicity. Ocrelizumab is the first monoclonal antibody for secondary primary progressive multiple sclerosis (PPMS)[1].
Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity[1][2][3].
Betulinic acid derivative-1 exhibits distinguished activities on inhibiting osteoclast (OC) differentiation with an IC50 value of 1.86 μM.
K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.IC50 value:Target: GATA-specific inhibitorin vitro: K-7174 inhibited the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either tumor necrosis factor alpha or interleukin-1beta, without affecting the induction of intercellular adhesion molecule-1 or E-selectin. K-7174 had no effect on the stability of VCAM-1 mRNA.K-7174 did not influence the binding to any of the following binding motifs: octamer binding protein, AP-1, SP-1, ets, NFkappaB, or interferon regulatory factor [1]. Addition of 10 microM K-7174 rescued these inhibitions of Epo protein production and promoter activity induced by IL-1beta, TNF-alpha, or L-NMMA, respectively [2]. K-7174 had the potential to induce endoplasmic reticulum (ER) stress evidenced by induction of GRP78 and CHOP.Other inducers of ER stress completely reproduced the effects of K-7174 including suppression of lipid accumulation, blockade of induction of adiponection and PPARgamma and maintenance of MCP-1 expression [3].in vivo: K-7174, one of proteasome inhibitory homopiperazine derivatives, exhibits a therapeutic effect, which is stronger when administered orally than intravenously, without obvious side effects in a murine myeloma model. Moreover, K-7174 kills bortezomib-resistant myeloma cells carrying a β5-subunit mutation in vivo and primary cells from a patient resistant to bortezomib [4].
BOS-318 is a potent, slowly dissociating, highly selective, and cell-permeable furin inhibitor with IC50 value of 1.9 nM. BOS-318 protects ENaC from subsequent activation by neutrophil elastase. BOS-318 can be used for the rsearch for CF lung disease[1][2].
Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist. IC50 value:Target: Histamine H1 receptorBepotastine Beslilate (Bepreve) also suppresses some allergic inflammatory processes such as allergic rhinitis, chronic urticaria or pruritus associated with skin conditions (eczema/dermatitis, prurigo or pruritus cutaneus).Bepotastine Beslilate (Bepreve) is useful for allergic conjunctivitis.
Sudoxicam is a reversible and orally active COX antagonist and a non-steroidal anti-inflammatory drug (NSAID) from the enol-carboxamide class. Sudoxicam has potent anti-inflammatory, anti-edema and antipyretic activity[1][2][3].
AQX-435 is a potent SHIP1 activator. AQX-435 reduces PI3K activation downstream of the B-cell receptor (BCR) and induces apoptosis of malignant B cells, and reduces lymphoma growth[1].
Isoengeletin is a flavonoid that can be isolated from the roots of Smilax bockii warb. Isoengeletin can be used as an active compound for the research of psoriasis, hyperuricemia and gout[1].
FR173657 is an orally active bradykinin B2 receptor antagonist (IC50: 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively). FR173657 (p.o.) inhibits BK-induced bronchoconstriction in guinea-pigs (ED50: 0.075 mg/kg). FR173657 (p.o.) also inhibits Carrageenin-induced paw oedema in mice (ED50: 6.8 mg/kg). FR173657 can be used for research of inflammatory disease[1].
Prodigiosin (Prodigiosine) hydrochloride is a red pigment produced by bacteria as a bioactive secondary metabolite. Prodigiosin hydrochloride is a potent proapoptotic agent, and inhibits Wnt/β-catenin pathway. Prodigiosin hydrochloride has antibacterial, antifungal, antiprotozoal, antimalarial, immunosuppressive, and anticancer properties[1][2].
WAY-169916 is a pathway-selective ligand of ER (estrogen receptor) that acts by inhibiting NF-kB transcriptional activity. WAY-169916 has potent anti-inflammatory effect[1].
2,6-Dimethoxy-1,4-benzoquinone, a natural phytochemical, is a known haustorial inducing factor. 2,6-Dimethoxy-1,4-benzoquinone exerts anti-cancer, anti-inflammatory, anti-adipogenic, antibacterial, and antimalaria effects[1].子
LEESGGGLVQPGGSMK, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α[1].
HDAC6-IN-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity[1].
Luteolin-7-rutinoside has both anti-arthritic and antifungal activities, can result in a combination therapy for the treatment of fungal arthritis due to C. albicans infection.
Wogonoside, a flavonoid glycoside isolated from Huangqin, possesses anti-inflammatory effects. Wogonoside induces autophagy in breast cancer cells by regulating MAPK-mTOR pathway[1][2].
β-Patchoulene is a tricyclic sesquiterpene isolated from the oil of Pogostemon cablin (patchouli oil). β-Patchoulene can be used for the treatment of inflammatory diseases[1].
Isoetharine (Isoetarine) mesylate is an orally active selective agonist of β-adrenergic receptors. Isoetharine mesylate is a catechol-like drug and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine mesylate can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator[1][2].
Lys-Gln-Ala-Gly-Asp-Val (KQAGDV) is the six most carboxyl-terminal amino acids in the fibrinogen γ-chain sequence. Lys-Gln-Ala-Gly-Asp-Val is a cell adhesion peptide which is mediated through the α2bβ3 integrin. Lys-Gln-Ala-Gly-Asp-Val is a potent adhesion ligand for smooth muscle cells (SMCs)[1][2].
Ligelizumab (QGE 031) is a humanized high-affinity monoclonal anti-IgE antibody. Ligelizumab can be used for the research of chronic spontaneous urticarial[1].
Blisibimod (A 623) is a potent and selective tetravalent inhibitor of B-cell activating factor (BAFF). Blisibimod can be used for the research of systemic lupus erythematosus (SLE)[1][2].
TMP778 is a potent and selevtive RORγt inverse agonist, with an IC50 of 7 nM in FRET assay.
ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'[1][2].
Alcindoromycin is an anthracycline antitumor antibiotic[1].