Resatorvid (TAK-242) is a potent TLR4 signaling inhibitor which selectively inhibits the TLR4-mediated production of cytokines and nitric oxide.
IL-1β-IN-1, cannabidiol derivative, is a potent IL-1β inhibitor. IL-1β-IN-1 has anti-inflammatory and pain-resolving properties[1].
Erepdekinra is an interleukin-17A (IL-17A) receptor antagonist[1].
NOS-IN-1 is a potent and orally active NO synthase (NOS) isoforms inhibitor with IC50s of 0.1 μM, 1.1 μM, and 0.2 μM for human iNOS (hiNOS), heNOS and hnNOS, respectively[1].
Lokivetmab (Anti-Canine IL31 Recombinant Antibody) is an anti-canine IL-31 monoclonal antibody that can be used for the research of atopic dermatitis (AD) in dogs[1].
Ppc-1 is a mitochondrial uncoupler. Ppc-1 enhances mitochondrial oxygen consumption without adverse effects on ATP production. Ppc-1 is a cell-permeate interleukin-2 (IL-2) inhibitor. Ppc-1 inhibits the Gram-negative periodontopathogen Porphyromonas gingivalis. Ppc-1 has anti-obesity, antibacterial and anti-inflammatory activities[1][2][3][4].
DB0614 (Example 21) is a bifunctional compound targeted protein degradation of kinases. DB0614 degrades AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK, LCK, LIMK2, MAP3KH, MAPK8, MAPK9, NEK9, PLK4, PTK2B, SIK2, STK17A, STK17B, ULK1, ULK3, and WEE1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity[1].
Withangulatin A is a selective cyclooxygenase-2 (COX-2) inhibitor. Withangulatin A can be isolated from Physalis angulata L. Withangulatin A has anti-tumor, trypanocidal activity and anti-inflammatory function[1].
AZ084 is a potent, selective, allosteric and oral active CCR8 antagonist, with a Ki of 0.9 nM. Has potential to treat asthma[1].
Longiferone B is a daucane sesquiterpene, that can be isolated from Boesenbergia longiflora rhizomes. Longiferone B shows anti-inflammatory activity against NO release with an IC50 of 21.0 μM. Longiferone B also suppresses the iNOS and COX-2 mRNA expression[1].
C3a receptor agonist 1 (compound benzeneacetamide) is a potent C3a receptor agonist. C3a receptor agonist 1 has the potential for the research of acute inflammation[1].
Cobitolimod is a DNA oligonucleotide agonist of TLR-9 with anti-inflammatory activity. Cobitolimod suppresses Th17 cells and induces anti-inflammatory FoxP3 and IL-10 expression, inhibiting the IL-17 signaling pathway[1].
L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with Kis of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS), respectively[1][2]. L-NIO dihydrochloride induces a consistentfocal ischemic infarctin rats[2].
Zeluvalimab (AMG-404) is a monoclonal antibody targeting the PD-1 receptor that can be used for the research of cancer[1].
BKT140 4-fluorobenzoyl is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM. Sequence: 4F-Benzoyl-Arg-Arg-{2-Naph-Ala}-Cys-Tyr-{Cit}-Lys-Lys-Pro-Tyr-Arg-{Cit}-Cys-Arg-NH2(Disulfide bridge: Cys4-Cys13).
ZK756326 is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.
Phenindamine (Nu 1504) is an antihistamine[1].
Olopatadine HCl is a histamine blocker used to treat allergic conjunctivitis.Target: Histamine ReceptorOlopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine significantly inhibited the ear swelling and the increased production of IL-4, IL-1beta, IL-6, GM-CSF and NGF in the lesioned ear [1]. Olopatadine was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine is one of the few renal clearance drugs in antiallergic drugs. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials [2]. AL-4943A inhibits histamine release in a concentration-dependent fashion (IC50 = 559 microM) from human conjunctival mast cell preparations in vitro. Passive anaphylaxis in guinea pig conjunctiva was attenuated by AL-4943A applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067% and 0.0170%, w/v, respectively) [3].
AZD4721 (RIST4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). AZD4721 has the potential for the research of inflammatory disease[1].
N-acetylhistamine is a histamine metabolite. N-acetylhistamine can be used as a potential biomarker of histidine metabolism for anaphylactoid reactions.
TLR7 agonist 4 (Compound 1.2) is a TLR7 agonist with an EC50 of 4.3 nM[1].
cGAMP(Cyclic GMP-AMP) is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA; STING ligand.Target:in vitro: cGAMP induced IFNβ RNA robustly even at concentrations as low as 10 nM. cGAMP was much more potent than c-di-GMP in inducing IFNβ based on ELISA assays. cGAMP was also more potent than c-di-GMP and c-di-AMP in activating IRF3. cGAMP binds to and activates STING to trigger the downstream signaling cascades [1]. On stimulation with cGAMP, fibroblasts from the patients showed increased transcription of IFNB1 but not of the genes encoding interleukin-1 (IL1), interleukin-6 (IL6), or tumor necrosis factor (TNF) [3]. cGAMP activates the endoplasmic reticulum (ER)-resident receptor STING, thereby inducing an antiviral state and the secretion of type I IFNs [4].in vivo: cGAMP can enhance the adaptive immune response to the model antigen ovalbumin in mice. cGAMP promotes antigen specific IgG and a balanced Th1/Th2 lymphocyte response in immunized mice [2].
Danicopan, a selective and orally active small-molecule factor D inhibitor, inhibits alternative pathway of complement (APC) activity. Danicopan has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS)[1].
Pozelimab (REGN3918) is a fully human IgG4 anti-C5 monoclonal antibody. Pozelimab binds to C5 and C5 variants with high affinity and blocks complement-mediated hemolysis. Pozelimab can be used for the research of complement-mediated diseases[1].
Triptoquinone A, an interleukin 1 inhibitor, inhibits endomycin (LPS) or interleukin (IL-1β)-promoted induction of nitric oxide synthase (NOS) in vascular smooth muscle, thereby inhibiting Arg-induced vascular relaxation[1].
Troxerutin, also known as vitamin P4, is a tri-hydroxyethylated derivative of natural bioflavonoid rutins which can inhibit the production of reactive oxygen species (ROS) and depress ER stress-mediated NOD activation.
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].
Betazole (Ametazole) dihydrochloride, a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole dihydrochloride induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole dihydrochloride has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity[1][2][3].
BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM)[1][2].
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.