Abetimus (LJP 394 free base) is an immunosuppressant consisting of four double-stranded DNA (dsDNA) oligonucleotides. Abetimus is capable of crosslinking anti-dsDNA antibodies on the surface of B cells, and decreases anti-dsDNA antibodies levels. Abetimus has the potential for research of systemic lupus erythematosus[1].
Uvaol, a triterpene present in olives and virgin olive oil, possesses anti-inflammatory properties and antioxidant effects. Uvaol attenuates pleuritis and eosinophilic inflammation in ovalbumin-induced allergy in mice[1].
Avasopasem manganese (GC4419; M-40419) is a potent superoxide dismutase mimetic that rapidly and specifically converts O2*- to hydrogen peroxide (H2O2), arresting the initiation of this cascade. Avasopasem manganese can be used for the research of severe oral mucositis (SOM) and cancer[1].
Niflumic Acid-d5 is the deuterium labeled Niflumic acid. Niflumic acid, a Ca2+-activated Cl- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis[1][2].
MART-1 (27-35) (human) is an immunogenic epitope recognized by HLA-A2-restricted melanoma-specific tumor-infiltrating lymphocytes (TIL)[1].
LY315920 (Varespladib) is a potent and selective human non-pancreatic secretory phospholipase A2 (sPLA) inhibitor with IC50 of 7 nM.IC50 value: 7 nMTarget: sPLA2in vitro: LY315920 exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50 of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively. [2] In BAL cells challenged with human sPLA2, LY315920 at doses ranging from 0.1 μM–3 μM reduces the formation of thromboxane mediated by human sPLA2 in a concentration-dependent manner with an IC50 of approximately 0.8 μM. [2] In human conjunctival epithelial cell line (HCjE), LY315920 (10 μM) significantly inhibits all-trans-retinoic acid (RA) -induced membrane-associated mucin MUC16 expression by 100% at 24 hours and 99% at 48 hours. [3]in vivo: Ex vivo, LY315920 at doses ranging from 3 mg/kg to 30 mg/kg via i.v. inhibits human sPLA2-induced release of thromboxane from guinea pig BAL cells with ED50 of 16.1 mg/kg. [2] In Transgenic Mice Expressing Human sPLA2, both oral and i.v. administration of LY315920 (0.3 mg/kg–3 mg/kg) abolishes serum sPLA2 activity in a dose and time dependent manner. [2]
Panepoxydone is an inhibitor of NF-κB activation. Panepoxydone interferes with the NF-κB mediated signal transduction by inhibiting the phosphorylation of IκB. Panepoxydone exhibits antitumor, anti-inflammatory, antimalarial and anti-parasitic activity[1][2].
Etofenamate-d4 is the deuterium labeled Etofenamate. Etofenamate, a non-steroid anti-inflammatory drug (NSAID) and a non-selective COX inhibitor, possesses analgesic, anti-rheumatic, antipyretic and anti-inflammatory properties. Etofenamate is used in the research for osteoarthritis, arthritis and other inflammatory diseases[1][2][3].
Moth Cytochrome C (MCC) (88-103), derived from the carboxyl terminus of moth cytochrome c, induces positive selection of TCR transgenic thymocytes[1].
Bendazac is an oxyacetic acid with anti-inflammatory, antinecrotic, choleretic and antilipidaemic properties. Bendazac acts by preventing protein denaturation and delays the cataractogenic process[1][2].
Vazegepant (BHV-3500) hydrochloride is a highly affinity CGRP receptor antagonist (hCGRP Ki= 0.023 nM). Vazegepant hydrochloride is the first intranasal gepant for migraine. Vazegepant hydrochloride may be helpful in effective management of COVID-19 associated pulmonary inflammation[1][2][3].
Deoxy artemisinin, a orally bioavailable compound separated from Artemisinin annua L., shows anti-inflammatory and antiulcer activities[1].
Reltecimod (AB-103) is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod can be used to research necrotizing soft-tissue infections (NSTIs)[1][2].
Uric acid-15N2 is the 15N labeled Uric acid[1]. Uric acid, scavenger of oxygen radical, is a very important antioxidant that help maintains the stability of blood pressure and antioxidant stress. Uric acid can remove reactive oxygen species (ROS) such as singlet oxygen and peroxynitrite, inhibiting lipid peroxidation[2][3].
Oct3/4-inducer-1 (compound 2) is a potent Oct3/4 inducer. Oct3/4-inducer-1 promotes expression and stabilization of Oct3/4, and enhances its transcriptional activity in diverse human somatic cells[1].
A novel potent, selective CDK8 inhibitor with IC50 of 0.5 uM against recombinant Cyclin C/CDK8 complex; displays no activity against several CDKs involved in cell cycle including CDK19 (IC50>30 uM); inhibits IFNγ-induced phosphorylation of STAT1 at Ser 727 site in BMDCs, selectively upregulates IL-10 with EC50 of 1 uM.
Chloranthalactone B, a lindenane-type sesquiterpenoid, is a nature product that could be isolated from Chinese medicinal herb Sarcandra glabra. Chloranthalactone B inhibits the production of inflammatory mediators by inhibiting the AP-1 and p38 MAPK pathways[1].
3-Oxo-7-hydroxychol-4-enoic acid is an endogenous metabolite. 3-Oxo-7-hydroxychol-4-enoic acid may be an important indicator of a poor prognosis in hepatobiliary disease[1].
Demeclocycline is an orally active tetracycline antibiotic. Demeclocycline impairs protein synthesis by binding to the 30S ribosomal subunit to inhibit binding of aminoacyl tRNA. Demeclocycline shows anti-bacterial activitise to a wide variety of bacterial infections[1][2].
Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM[2]. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca2+ transport with an IC50 of 140 nM in a Ca2+ uptake assay[1]. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway[4]. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease[5].
Thromboxane A2 (TXA2) is a prostanoid mediator produced by the metabolism of Arachidonic acid (HY-109590) through the cyclooxygenase pathway. Thromboxane A2 activates the thromboxane-prostanoid (TP) receptors. Thromboxane A2 is a potent vasoconstrictor eicosanoid. Thromboxane A2 (TXA2) leads to potent vasoconstriction by stimulation of smooth muscle cells. Thromboxane A2 acts as s tonic immunoregulator to regulate adaptive immune responses[1][2].
ENMD-1068 hydrobromide is a potent PAR2 antagonist. ENMD-1068 hydrobromide attenuates joint inflammation in a dose-dependent manner. ENMD-1068 hydrobromide can be used in research of joint inflammation[1].
Diammonium Glycyrrhizinate, isolated from the licorice root, is a widely used anti-inflammatory agent[1].
PKC-IN-4 (compound 7l) is a potent and orally active aPKC inhibitor with an IC50 of 0.52 µM. PKC-IN-4 inhibits TNF-α induced NF-κB activity in vitro. PKC-IN-4 blocks VEGF- and TNFα-induced permeability across the retinal vasculature[1].
(R)-Elexacaftor is an enantiomer of Elexacaftor (HY-111772). (R)-Elexacaftor is the Compound 37 from patent WO2018107100A1. (R)-Elexacaftor is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR), the EC50 for CFTR dF508 is 0.29 uM[1].
Robenacoxib is a nonsteroidal anti-inflammatory and analgesic agent. Robenacoxib is a selective COX-2 inhibitor[1][2].
Amdizalisib is a PI3K inhibitor and used for the research of inflammatory disease, autoimmune disease or cancer[1].
Trabikibart (CSL311), a βc-specific, fully human monoclonal antibody, binds to a unique epitope that is specific to the cytokine-binding site of the human βc receptor. Trabikibart has picomolar binding affinity for the human βc receptor. Trabikibart is a potent inhibitor of the combined effects of IL-3, GM-CSF and IL-5 on the survival of eosinophils. Trabikibart has the potential for chronic inflammatory diseases research[1].
Notopterol is a coumarin extracted from N. incisum. Notopterol induces apoptosis and has antipyretic, analgesic and anti-inflammatory effects. Notopterol is used for acute myeloid leukemia (AML)[1].
Caffeic acid phenethyl ester is a NF-κB inhibitor.