EGTA is a specific calcium ion chelator. EGTA has an apparent calcium dissociation constant (Kd) of 60.5 nM at physiological pH (7.4) and has very high specificity for Ca2+ over Mg2+ (Mg2+ Kd 1-10 mM). EGTA significantly inhibited the substrate adherence capacity of inflammatory macrophages[1][2].
ALR-27 is an antagonist of the 5-lipoxygenase (5-LOX) activating protein FLAP and has anti-inflammatory activity. ALR-27 potently inhibits 5-LOX product formation (>80%) in pro-inflammatory M1-MDM, with no significant direct inhibition of 5-LOX. ALR-27 not only reduces prostaglandin and leukotriene (LT) production in neutrophils but also increases the production of specialized prolytic mediators in specific human macrophage phenotypes[1].
Tafasitamab is an Fc-modified, humanized monoclonal antibody that binds to the human B-cell surface antigenCD19[1][2].
6,7,8-Trihydroxy-2-(2-Phenethyl) chromone is a chromone derivative with anti-inflammatory effects[1].
URAT1 inhibitor 1 (1g) is a uric acid transporter 1 (URAT1) inhibitor, with an IC50 of 32 nM. URAT1 inhibitor 1 has potential to treat hyperuricemia associated with gout[1].
SB 203580 hydrochloride is a widely used p38 MAPK inhibitor with an IC50 of 0.3-0.5 μM. It shows more than 100-fold selectivity over PKB, LCK, and GSK-3β.
Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α’s RNase[1].
Relfovetmab is an anti-NGF monoclonal antibody (mAb)[1].
BCX 1470 inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.IC50 Value: 96 nM (Factor D); 1.6 nM (C1s); 326 nM (Trypsin) [1]Target: Factor D; C1sBCX 1470(Thrombin inhibitor) is serine protease inhibitor.BCX 1470(Thrombin inhibitor) blocks the esterolytic and hemolytic activities of the complement enzymes Cls and factor D in vitro, also blocked development of RPA-induced edema in the rat.
CMS-121 is a quinolone derivative and an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor. CMS-121 protects HT22 cells against ischemia and oxidative damage with EC50 values of 7 nM and 200 nM, respectively. CMS-121 has strong neuroprotective, anti-inflammatory, antioxidative and renoprotective activities[1][2][3].
Bepotastine is an orally active second-generation histamine H1 receptor antagonist. Bepotastine has the potential for allergic rhinitis and urticaria/pruritus treatment[1][2].
20-Hydroxyganoderic Acid G is a lanostane triterpenoid obtained from the EtOH extract of fruiting bodies of the Ganoderma curtisii. 20-Hydroxyganoderic Acid G inhibits BV-2 microglia cells activated by LPS with an IC50 of 21.33 μM. 20-Hydroxyganoderic Acid G has therapeutic potential in the drug discovery of nerve inflammation diseases associated with microglia activated by LPS[1].
Tremelimumab (Ticilimumab) is a fully humanized monoclonal antibody specific for cytotoxic T-lymphocyte antigen-4 (CTLA-4) and can be used for metastatic melanoma research[1].
(S,R,S)-AHPC-C5-NH2 hydrochloride (VH032-C5-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C5-NH2 hydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1[1].
Cetylpyridinium chloride, a cationic quaternary ammonium compound, is an anti-bacterial agent with broad-spectrum activity. Cetylpyridinium chloride is an effective anti-HBV capsid assembly inhibitor with an IC50 of 2.5 μM. Cetylpyridinium chloride is used in pesticides and various types of mouthwashes, and other personal care products[1][2].
Mavrilimumab (CAM 3001) is a monoclonal antibody that binds to the α subunit of the granulocyte-macrophage colony stimulating factor (GM-CSF) receptor and blocks intracellular signalling downstream of GM-CSF. GM-CSF might be a mediator of the hyperactive inflammatory response associated with respiratory failure and death[1].
Norisoboldine is an isoquinoline alkaloid which acts as an AhR agonist, and enhances the function of the adenosine A1 receptor.
Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis[1][2][3].
AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors.IC50 Value: ~3 nM (EC50 for calcium mobilization by PGE2) [1]Target: EP/DP receptorin vitro: AH6809also antagonized the aggregatory effect of U-46619 in whole blood (pA2 = 4.45). However, concentrations of AH6809 up to 300 microM were without effect upon either ADP- or platelet activating factor (Paf)-induced aggregation (pA2 less than 3.5) [2]. Preincubation of control cells in 10(-4) M concentrations of AH6809 inhibited PGE2-induced activation of AC by greater than 80% without significant (P greater than .05) inhibition of basal activity by the antagonist [3].in vivo: Exposure to a selective COX-2 inhibitor (SC58125) or an EP1/EP2 antagonist (AH6809), but not an EP4 antagonist (AH23848B), significantly reduced cell proliferation of esophageal explants in 24 hour-organ culture experiments [4]. Oral administration of the EP1 receptor antagonist, AH6809 (10 mg/kg/day, for 4 days), significantly reduced the systolic blood pressure in db/db, but not in control mice [5].
Helenalin is an anti-inflammatory sesquiterpene lactone. Helenalin selectively inhibits transcription factor NF-κB by directly targeting p65. Helenalin has alkylating activity, targets the cysteine sulfhydryl groups in the p65 subunit of NF-κB, thereby inhibits its DNA binding[1][2].
Bevenopran is a peripheral μ-opioid receptor antagonist.
C-Reactive Protein (CRP) 201-206 is the 201-206 fragment of C-Reactive Protein. C-Reactive Protein (CRP), the prototypic marker of inflammation, is a cardiovascular risk marker and may promote atherogenesis[1].
Chrysosplenol D is a methoxy flavonoid that induces ERK1/2-mediated apoptosis in triple negative human breast cancer cells. Chrysosplenol D also exhibits anti-inflammatory and moderate antitrypanosomal activities[1][2][3][4].
Neotuberostemonine, one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, attenuates bleomycin-induced pulmonary fibrosis by suppressing the recruitment and activation of macrophages[1].
C5aR-IN-3 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-3 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 89)[1].
Sephin 1 (NSC 65390) is a selective inhibitor of PPP1R15A that disrupts the PPP1R15A-PP1c complex but spares the related PPP1R15B-PP1c complex; prolongs eIF2α phosphorylation after stress, attenuates the expression of stress genes such as CHOP, and protects cells from cytotoxic ER stress; lacks any measurable α2-adrenergic agonist activity in a cell-based assay, in contrast to Guanabenz; safely prevents the motor, morphological, and molecular defects in mice.
Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[2]. Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment[5].
AMT hydrochloride is a selective inhibitor of inducible NOS (iNOS) with Ki of 4.2 nM[1].
25S-Inokosterone is a phytoecdysone in the roots of two same species of A. bidentata Blume and A. japonica Nakai, and two different species of C. capitata Moq and C. officinalis Kuan. 25S-Inokosterone has the potential for the LPS-induced acute kidney injury research[1][2].
Asarylaldehyde is a natural COX-2 inhibitor, which isolated from carrot (Daucus carota L.) seeds significantly inhibits cyclooxygenase II (COX-2) activity at IC50 value 100 μg/mL.