Bermekimab (MABp1) is a human monoclonal antibody that targets interleukin-1alpa (IL-1α). Bermekimab prevents tumour-related inflammation[1].
Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
Anti-inflammatory agent 46 (compound 7h) is an anti-inflammatory agent with nitric oxide (NO) inhibitory effect. Anti-inflammatory agent 46 binds to iNOS with low energies, inhibits swelling in mice (at dose of 10 mg/kg)[1].
c-JUN peptide is a cell-permeable c-JUN-JNK interaction inhibitor. c-JUN peptide inhibits serum-induced c-Jun phosphorylation. c-JUN peptide induces apoptosis[1].
Revaprazan (SB 641257) is a reversible proton pump inhibitor with significant anti-inflammatory effects. Revaprazan can be used for chronic gastric inflammation research[1][2].
Brombuterol D9 hydrochloride (Bromobuterol D9 hydrochloride) is a deuterium labeled Brombuterol hydrochloride. Brombuterol hydrochloride is a β-adrenergic receptor agonist[1].
FN-439 is a selective collagenase-1 inhibitor. FN-439 inhibits collagenase-1 with an IC50 value of 1 μM. FN-439 can be used for the research of cancer and inflammation[1][2].
SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 μM).IC50 value:Target: p38 MAPK inhibitorin vitro: SKF-86002 inhibited prostaglandin H2 (PGH2) synthase activity (IC50 120 microM) as well as prostanoid production by rat basophilic leukemia (RBL-1) cells (IC50 70 microM) and its sonicate (IC50 100 microM) and human monocytes (IC50 1 microM). In addition, SK&F 86002 inhibited the generation of dihydroxyeicosatetraenoic acid (diHETE) and 5-hydroxyeicosatetraenoic acid (5-HETE) by a high speed supernatant fraction of RBL-1 cells (IC50 10 microM) [1]. differentiation of HL-60 cells toward the neutrophil phenotype resulted in a loss in c-Jun NH2-terminal kinase activation with concomitant acquisition of formylmethionylleucylphenylalanine-stimulatable and stress-inducible p38 MAPK activity as well as apoptosis blockade by SKF-86002 [2]. SKF-86002 blocked superoxide anion production in response to FMLP and reduced adhesion and chemotaxis in response to PAF or FMLP [3].
VAF347 is a cell permeable and highly affinity aryl hydrocarbon receptor (AhR) agonist and induces AhR signaling. VAF347 inhibits the development of CD14+CD11b+ monocytes from granulo-monocytic (GM stage) precursors. VAF347 has anti-inflammatory effects[1].
12-Epinapelline is a diterpene alkaloid isolated from Aconitum baikalense. 12-Epinapelline exhibits Anti-inflammatory activity and stimulates the growth of colonies from fibroblast precursors[1][2].
RXFP1 receptor agonist-5 (Example 98) is a RXFP1 receptor agonist. RXFP1 receptor agonist-5 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 1.3 nM[1].
10-Hydroxy-2-decenoic acid (10-HDA) is the major lipid component of royal jelly produced by honeybees. 10-Hydroxy-2-decenoic acid has several health-beneficial effects in mammals, such as antitumor activity, anti-inflammatory activity, and antiangiogenic activity. 10-Hydroxy-2-decenoic acid also extends the lifespan of C. elegans[1].
Trafermin is a recombinant human basic fibroblast growth factor (rhbFGF). Trafermin is a potent FGFR inhibitor. Trafermin improves degree of re-epithelialization. Trafermin can be used in research in skin healing[1].
IKK2-IN-3 (Compound 8) is an IKK2 inhibitor with an IC50 of 0.075 μM[1].
PF-00356231 hydrochloride is a specific, non-peptidic, non-zinc chelating ligand and inhibitor of matrix metalloproteinase MMP-12 (IC50=1.4 μM). PF-00356231 hydrochloride binds to MMP-12 and forms PF-00356231/MMP-12 complex. PF-00356231 hydrochloride shows potency against MMP-13, MMP-8, MMP-9, MMP-3 with IC50s of 0.00065, 1.7, 0.98, 0.39 μM, respectively[1].
Protoplumericin A is a bioactive ingredient of Plumeria obtusa L. attenuates. Protoplumericin A mitigated lipopolysaccharide (LPS) -induced acute lung injury in mice. Protoplumericin A can be used to study the LPS-induced anti-inflammatory effect [1].
Mefenamic Acid-d3 is the deuterium labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
Quercitrin is a natural compound found in Tartary buckwheat with a potential anti-inflammation effect that is used to treat heart and vascular conditions.IC50 value:Target:In vitro: There were significant increases in caspase-3 activity, loss of MMP, and increases in the apoptotic cell population in response to quercitrin in DLD-1 colon cancer cells in a time- and dose-dependent manner. [1] In vivo: ICR mice received CCl4 intraperitoneally with or without quercitrin co-administration for 4 weeks. Data showed that quercitrin significantly suppressed the elevation of reactive oxygen species (ROS) production and malondialdehyde (MDA) content, reduced tissue plasminogen activator (t-PA) activity, enhanced the antioxidant enzyme activities and abrogated cytochrome P450 2E1 (CYP2E1) induction in mouse brains. [2]
STING agonist-10 (Compound 91) is a potent small molecule cyclic urea activator of STING with the EC50 of 2600 nM. Activation of STING is a highly promising approach in immunotherapy[1].
CL2A-SN-38, SN-38 (topoisomerase-I inhibitor) derivative, is a peptide linker. CL2A-SN-38 is conjugated to the anti-Trop-2-humanized antibody, SN-38-anti-Trop-2 antibody-drug conjugate (ADC) against several human solid tumor types, provides significant and specific antitumor effects against a range of human solid tumor types[1].
WKYMVM (TFA) is a potent N-formyl peptide receptor (FPR1) and FPRL1/2 agonist, also activates several leukocyte effector functions such as chemotaxis, mobilization of complement receptor-3, and activation of the NADPH oxidase[1][2].
Succinobucol is a phenolic antioxidant with anti-inflammatory and antiplatelet effects.
Methyl 2-acetoxybenzoate (Methyl acetylsalicylate) is a safe and simple anti-inflammatory aspirin prodrug. Methyl 2-acetoxybenzoate (Methyl acetylsalicylate) can be chemical or enzymatically hydrolysed to methyl 2-hydroxy benzoate. Methyl 2-acetoxybenzoate (Methyl acetylsalicylate) can be used as analgesic agent in liniments and also inflammatory diseases research[1].
E6446 dihydrochloride is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses.
(-)-Bornyl ferulate is a 5-lipoxygenase and COX inhibitor with IC50s of 10.4 μM and 12.0 μM, respectively[1].
DW-1350 is a LTB4 receptor antagonist.
Massonianoside B is an antioxidant, which can be isolated from Cedrus deodara pine needle. Massonianoside B exhibits radicals scavenging capacities, and restores CCL4-impaired activity of antioxidant enzymes[1].
IL-17 modulator 2 (compound 159) is an orally active modulator of IL-17. IL-17 modulator 2 significantly reduces IL-6, IFN-γ, and edema. IL-17 modulator 2 can used in study arthritis[1].
(+)-Pinoresinol diacetate is an antifungal agent that can be isolated from Sambucus williamsii[1].
CB2 modulator 1 (compound 130) is a potent CB2 modulator. CB2 modulator 1 has the potential for immunedisorders, inflammation, osteoporosis, renal ischemia[1].