3-Oxo-hop-22(29)-ene is a yeast α-glucosidase inhibitor. 3-Oxo-hop-22(29)-ene shows a moderate effect on the viability of T. cruzi and L. mexicana. 3-Oxo-hop-22(29)-ene shows marginal activity of anti-inflammatory[1].
4''-methyloxy-Genistin, an isoflavone methyl-glycoside, is isolated from Cordyceps militaris grown on germinated soybeans. Isoflavones possess immunomodulating and antiallergic activities[1].
3,3-Diaminobenzidine tetrahydrochloride dehydrate is a staining agent that is often used in histochemical (HC) and immunohistochemical (IHC) procedures. 3,3-Diaminobenzidine tetrahydrochloride dehydrate can be used for peroxisomal staining and mitochondrial cytochrome c oxidase activity staining[1].
CGP-35949 sodium is a LTD4 antagonist with phospholipase inhibitory activity. CGP-35949 sodium can be used for research of asthma[1].
Morolimumab is an IgG1 human anti-RHD/CD240D monoclonal antibody. Morolimumab can be used for the research of immune disease[1].
Patamostat (E-3123) is a potent protease inhibitor. Patamostat potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. E-3123 may possess suppressing effects on pathogenesis and development of acute pancreatitis[1][2].
Zabedosertib (BAY 1834845) is a IRAK4 inhibitor with immunomodulatory potential. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors[1].
ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter[1][2][3].
Capsiconiate (Coniferyl (E)-8-methyl-6-nonenoate) is a TRPV1 agonist (EC50= 3.2 μM). Capsiconiate can be used to study TRPV1-mediated diseases such as pain, inflammation, and epilepsy(EC50= 3.2 μM)[1].
CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD)[1].
ChemR23-IN-4 (Compound 13) is a potent and orally efficacious ChemR23 inhibitor with an IC50 of 17 nM against human ChemR23[1].
Myricetin 3-O-glucoside (Myricetin 3-β-D-glucopyranoside) is a flavonol from Tibouchina paratropica. Myricetin 3-O-glucoside exhibits anti-Leishmanial, anti-inflammatory and antimicrobial activities[1].
Cbl-b-IN-13 (Example 520) is a Cbl-b inhibitor with an IC50 of <100 nM. Cbl-b-IN-13 has the ability to activate T-cells[1].
P18IN003 is a potent p18(INK4C) inhibitor andspecifically block the activity of p18 protein. P18IN003 has the potential to be aneffective chemical agent for therapeutic expansion of HSC[1].
Deoxysappanone B (3-Deoxysappanone B) is a homoisoflavone compound isolated from Caesalpinia sappan L (Lignum Sappan). Deoxysappanone B has anti-neuroinflammatory and neuroprotective effects and inhibits the production of neuroinflammatory mediators by blocking the IκB kinase (IKK)-NF-κB and p38/ERK MAPK pathways. Deoxysappanone B can be used in disease studies of neuritis and inflammation-related neurological damage[1].
Tripelennamine citrate, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine citrate lessens the allergic response of the organism caused by histamine. Tripelennamine citrate can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions[1][2][3].
hIgG–hFc receptor-IN-1 (comp 66) is a human immunoglobulin G–human neonatal Fc receptor (hIgG–hFcRn) protein-protein interaction inhibitor, with an IC50 of 2 μM [1].
Tetramethylcurcumin (FLLL31), derived from curcumin, specifically suppresses the phosphorylation of STAT3 by binding selectively to Janus kinase 2 and the STAT3 Src homology-2 domain. Tetramethylcurcumin exhibits anti-inflammatory and anti-cancer effects[1][2].
Sugiol is an abietane diterpenoid, can be isolated from Calocedrus formosana bark. Sugiol has anti-inflammatory activity, could effectively reduce intracellular reactive oxygen species (ROS) production in lipopolysaccharide (LPS)-stimulated macrophages[1].
Junceellolide C is a transcription inhibitor of cccDNA. Junceellolide C inhibits HBV DNA replication and significantly decreases the level of supernatant HBV RNA with EC50 values of 5.19, 3.52 μM respectively in HepAD38 cells. Junceellolide C is a potent anti-HBV agent[1].
MrgprX2 antagonist-5 is an MrgprX2 antagonist extracted from patent WO2020223255A1, example 16. MrgprX2 antagonist-5 can be used for the research of inflammatory disorders of the skin[1].
BML-280 (VU0285655-1) is a potent and selective phospholipase D2 (PLD2) inhibitor. BML-280 has the ability to prevent caspase-3 cleavage and reduction in cell viability induced by high glucose. BML-280 can be used for rheumatoid arthritis research[1][2].
Kushenol B is an isoprenoid flavonoid isolated from S. flavescens, has antimicrobial, anti-inflammatory and antioxidant activities[1]. Kushenol B has inhibitory activity against cAMP phosphodiesterase (PDE), with an IC50 of 31 µM[1].
Azido-PEG9-acid is a non-cleavable 9 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
RN486 is a selective Btk inhibitor with an IC50 Value of 4.0 nM.IC50 Value: 4.0 nM [1]Target: Btk Kinasein vitro: In the enzymatic assay, the compound potently inhibited Btk kinase activity with an IC50 of 4.0 nM. RN486 not only potently and selectively inhibited the Btk enzyme, but also displayed functional activities in human cell-based assays in multiple cell types, blocking Fcε receptor cross-linking-induced degranulation in mast cells (IC(50) = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC(50) = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC(50) = 21.0 nM) [1]. In a co-culture system consisting of human primary synovial FLS and activated human platelets, convulxin stimulation resulted in elevated production of pro-inflammatory cytokines, IL-6 and IL-8, an effect which was dose-dependently blocked by RN486 [2].in vivo: RN486 displayed similar functional activities in rodent models, effectively preventing type I and type III hypersensitivity responses. More importantly, RN486 produced robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibited both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood [1]. The administration of RN486 completely stopped disease progression, as determined by histologic and functional analyses of glomerular nephritis. The efficacy was associated with striking inhibition of B cell activation, as demonstrated by a significant reduction in CD69 expression in response to BCR crosslinking. RN486 markedly reduced the secretion of IgG anti-double-stranded DNA (anti-dsDNA) secretion, as determined by enzyme-linked immunosorbent and enzyme-linked immunospot assays [3].
Nocloprost, a prostaglandin E2 (PGE2) analog, is an orally active EP1- and EP3-receptor agonist. Nocloprost inhibits evoked [3H]ACh release. Nocloprost has gastroprotective and ulcer-healing properties. Nocloprost accelerates the healing of chronic gastric ulcerations and enhances mucosal growth in rats[1][2].
TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.IC50 value: 7.1 nM [1]Target: p38α MAPKin vitro: TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM [1]. TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells [2]. The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop [3].in vivo: TAK 715 (10 mg/kg, po) inhibits LPS-induced TNF-alpha production in mice with 87.6% inhibition. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 results in Cmax of 0.19 μg/mL and AUC(0-24 hours) of 1.16 μg·h/mL in rats. TAK 715 (30 mg/kg, po) significantly reduces the secondary paw volume with 25 % inhibition in a rat adjuvant-induced arthritis (AA) model [1].
Dimethoxycurcumin is a derivative of curcumin that has anti-inflammatory and antioxidant activities[1][2].
Xanthoxyletin is a coumarin that can be isolated from Genus Zanthoxylum and Clausena. Xanthoxyletin has antioxidant and anti-inflammatory activities. Xanthoxyletin shows cytotoxic effects to cancer cells, and induces apoptosis and necrosis. Xanthoxyletin can be used for the research of cancer and inflammation[1][2].
(-)-Epigallocatechin Gallate is an antioxidant polyphenol flavonoid form green tea, and inhibits the activation of EGFR, HER2 and HER3, with antitumor activity.