Ciwujianoside D1 is a natural product that can inhibit histamine release induced by anti-immunoglobulin E from rat peritoneal mast cells[1].
SB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC50 of 4.5 nM[1].
2,5-Dihydroxyacetophenone, isolated from Rehmanniae Radix Preparata, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways[1].
Fargesone A is a potent and selective FXR agonist. Fargesone A shows anti-inflammatory activity[1].
Cytochrome c-pigeon (88-104) (PCC 88-104) has full stimulatory activity for pigeon cytochrome c-primed T cells from B10.A mice. The I-Ek-restricted T cell response to Cytochrome c pigeon (pcyt c) is specific for the COOH-terminal sequence 88-104[1][2].
Pegademase bovine (PEG-ADA) is an enzyme product. Pegademase bovine can be used for the research of severe combined immunodeficiency (SCID) such as adenosine deaminase deficiency (ADA) [1].
Norethindrone acetate is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
LCMV gp33-41 is the H-2Db restricted epitope derived from the lymphocytic choreomeningitis virus (LCMV) glycoprotein gp 33; residues 33 to 41.
Viscidulin II (FL6) is a flavone. Viscidulin II can be isolated from the root of Scutellaria baicalensis. Viscidulin II significantly suppresses P. acnes-induced IL-8 and IL-1β production in THP-1 cells[1].
Clobutinol is a compound that has anti-tussive effects. Clobutinol affects heart rate and blood pressure, it can be used for cough related research[1][2][3].
UAMC-00050 is a potent trypsin-like serine protease inhibitor. UAMC-00050 can be used in research of dry eye syndrome and ocular inflammation[1].
(-)-Ketoconazole is one of the enantiomer of Ketoconazole. Ketoconazole is a racemic mixture of two enantiomers, levoketoconazole ((2S,4R)-(−)-ketoconazole) and dextroketoconazole ((2R,4S)-(+)-ketoconazole).
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine has a multi-path anti-fibrosis function and a renal protection function for research of renal anemia[1].
Kifunensine, a potent and selective inhibitor of class I α-mannosidases isolated from Actinomycete, prevents α-mannosidases I from trimming mannose residues on glycoproteins. Kifunensine inhibits ERAD[1][2][3].
Dihydromyristicin, a plant flavonoid, has potent anti-inflammatory properties. Dihydromyristicin reduces endotoxic inflammation via repressing ROS-mediated activation of PI3K/Akt/NF-κB signaling pathways[1].
TGFβ-IN-2 (Compound 9d) inhibits TGF-β-induced total collagen accumulation in NRK-49F cells with the IC50 of 4.31 μM. TGFβ-IN-2 suppresses the TGF-β-induced protein expression of COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 can be used as a potential effective compound for anti-fibrosis in vivo by oral administration[1].
Meseclazone exhibits inhibitory potency of secondary phase ADP aggregation. Meseclazone possesses anti-inflammatory, analgesic and antipyretic activity.
Rontalizumab (RhuMab IFNalpha) is a humanized IgG1 monoclonal antibody targets IFN-α. Rontalizumab can be used for the research of systemic lupus erythematosus[1].
XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2[1]. XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules[2].
PF-06260933 is a highly selective small-molecule inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively.
Simtuzumab (AB 0024; GS 6624) is a monoclonal antibody directed against Lysyl oxidase like-2 (LOXL2). Simtuzumab can be used for the research of primary sclerosing cholangitis (PSC)[1].
RORγt agonist 2 is a potent agonist of RORγt. RORγt agonist 2 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 2 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136339A1, compound 17)[1].
Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive[1][2].
SPD304 dihydrochloride is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α[1][2].
Balsalazide sodium hydrate could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
PKCβII Peptide Inhibitor I is a PKCβII inhibitor. PKCβII Peptide Inhibitor I shows cardioprotective effects in rat cardiac Ischemia/reperfusion injury model. PKCβII Peptide Inhibitor I also prevents vascular endothelial dysfunction[1].
Zardaverine is a newly developed dual-selective PDE3/4 inhibitor with IC50 values of 0.5 uM and 0.8 uM respectively. IC50 value: 0.5 uM (PDE3); 0.8 uM (PDE4)Target: PDE3; PDE4Zardaverine inhibited the cyclic GMP-inhibitable PDE III from human platelets and the rolipram-inhibitable PDE IV from canine trachea and human polymorphonuclear (PMN) cells with IC50-values of 0.58, 0.79 and 0.17 μM, respectively. The pyridazinone derivative affected the calmodulin-stimulated PDE I, the cyclic GMP-stimulated PDE II and the cyclic GMP-specific PDE V only marginally at concentrations up to 100μM. Zardaverine inhibits the ADP-induced aggregation of human platelets with an IC50 of 1.6 μM. This inhibition was synergistically increased by activators of adenylate cyclase such as PGE1 and forskolin. In human PMN cells, Zardaverine inhibited the zymosan-induced superoxide anion generation with an IC50 of 0.40 μM. Again, this effect was increased by activators of adenylate cyclase. Zardaverine acted in synergy with the adenylate cyclase activators prostaglandin E2 and CG 4203, a prostacyclin analog, and super-additive effects of combinations were observed. Zardaverine and dexamethasone prevent bronchial eosinophilia and neutrophilia with similar dosage of 30 microM/kg orally, suggesting that this PDE III/IV inhibitor may be useful for both, bronchorelaxation and reduction of inflammation in asthma therapy.
Brevifolincarboxylic acid is extracted from Polygonum capitatum[1], has inhibitory effect on the aryl hydrocarbon receptor (AhR)[2]. Brevifolincarboxylic acid is an α-glucosidase inhibitor with an IC50 of 323.46 μM[3].
4-Acetoxycinnamic acid is an acetate ester obtained by the formal condensation of the hydroxy group of trans-4-coumaric acid with acetic acid. 4-Acetoxycinnamic acid is a member of cinnamic acids and a member of phenyl acetates. 4-Acetoxycinnamic acid derives from a trans-4-coumaric acid[1].
3-O-Methylviridicatin is an inhibitor of TNF-α.3-O-Methylviridicatin inhibits TNF-a synthesis instead of the activity. 3-O-Methylviridicatin can be used in study anti-in?ammatory agents[1].