Cemiplimab (Anti-Human PD-1) is a high-affinity programmed death receptor-1 (PD-1) monoclonal IgG4 antibody that blocks PD-1/PD-L1-mediated T-cell suppression. Cemiplimab is commonly used in squamous cell skin cancer research[1][2].
MCC950 is a potent and selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
Enflicoxib (E 6087) is a nonsteroidal anti-inflammatory compound that selectively inhibits cyclooxygenase-2 (COX-2). Enflicoxib does not inhibit cyclooxygenase-1 (COX-1). E-6087 shows anti-inflammatory, analgesic and antipyretic activities in animal models[1].
COX-2-IN-24 is an orally active inhibitor of COX-2 with IC50 value of 0.17 μM, shows anti-inflammatory and low ulcerogenic activities.
Fenspiride Hcl is an α adrenergic and H1 histamine receptor antagonist.IC50 value:Target: Adrenergic receptor; H1 receptorFenspiride hydrochloride is a bronchodilator with anti-inflammatory properties. Fenspiride hydrochloride inhibits mucus secretion and reduces the release of tachykinins at a prejunctional level. Fenspiride hydrochloride also may be an antagonist at α adrenergic and H1 histamine receptors.
Schiarisanrin A (Kadsulignan J) is a lignan with inhibitory activity on NO production. Schiarisanrin A inhibits NO production in BV-2 cells with an IC50 of 9.6 μM[1].
Methapyrilene is a histamine antagonist, a pyridine chemical with anticholinergic activity. Methapyrilene can cause target organ-specific epigenetic alterations, such as a decrease in DNA methylation levels. Methapyrilene induces hepatocellular carcinoma in rats[1][2].
Terfenadine-d3 ((±)-Terfenadine-d3) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM[1]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].
Oxyphenbutazone monohydrate is a Phenylbutazone (HY-B0230) metabolite, with anti-inflammatory effect. Oxyphenbutazone monohydrate is an orally active non-selective COX inhibitor. Oxyphenbutazone monohydrate selectively kills non-replicating Mycobaterium tuberculosis[1][2].
Briakinumab (ABT-874) is a fully human anti-IL-12/23p40 monoclonal antibody. Briakinumab targets and neutralizes IL-12 and IL-23. Briakinumab can be used for the research of rheumatoid arthritis, inflammatory bowel disease, and multiple sclerosis[1].
CCR6 antagonist 1 is a CCR6 antagonist that inhibits the CCL20/CCR6 axis. CCR6 antagonist 1 can be used in the research of autoimmune-mediated inflammatory diseases, such as inflammatory bowel diseases (IBDs)[1].
COX/5-LOX-IN-1 (compound 6b) is a potent and dual inhibitor of COX/5-LOX with IC50s of 1.07, 0.55, and 0.28 μM for COX-1, COX-2, and 5-LOX enzyme, respectively. COX/5-LOX-IN-1 has the potential for the research of inflammation diseases[1].
S-Nitroso-N-acetyl-DL-penicillamine (SNAP) is a nitric oxide donor and acts as a stable inhibitor of platelet aggregation[1][2][3][4].
CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1[1].
MSA-2 is an orally available non-nucleotide STING agonist, with EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 shows antitumor activity and stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models[1].
C5a Receptor agonist, mouse, human is a biological active peptide. (This peptide is derived from the C-terminus of the chemokine, complement fragment 5 anaphylatoxin (C5a). This peptide functions as a C5a receptor agonist. C5a is a plasma protein involved in cellular inflammatory processes by inducing chemotaxis, degranulation of leukocytes, increased vascular permeability, and cytokine production. The cyclohexylalanine at position 5 is crucial to agonist function. Arg at the last position is of the d-isomer.)
HTMT (dimaleate) is a potent histamine H1 and H2 receptor agonist. HTMT (dimaleate) is 4 x 104 times more active than histamine in H2-mediated effects in natural suppressor cells[1].
ODN 1826, a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. CpG ODN 1826 is an excellent immunostimulator that induces NO and iNOS production in the murine model. CpG ODN 1826 enhances cell apoptosis. ODN 1826 sequence: 5’-tccatgacgttcctgacgtt-3’[1][2][3].
Ginsenoside Rb3 is extracted from steamed Panax notoginseng. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
Tripelennamine, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine lessens the allergic response of the organism caused by histamine. Tripelennamine can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions[1][2][3].
Chloranthalactone E (compound 6), a labdane diterpene, can be isolated from the aerial parts of Chloranthus serratus. Chloranthalactone E inhibits NO production in LPS-activated RAW 264.7 macrophages[1].
J-113863 is a potentand selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 has no active against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect[1][2][3].
N4-Acetylcytidine triphosphate is a endogenous nucleoside metabolite from the degradation of tRNA, primes and activates NLRP3 inflammation by inducing HMGB1 expression[1].
TLR7 agonist 7 (compound IIb-26) is an TLR7 agonist with an EC50 value of ~4 nM[1].
ODN 6016 is a CpG-A oligonucleotides. ODN 6016 can induce IFN-α production, can be used for researching immune disorders including immunodeficiency caused by HIV-1. ODN 6016 sequence: T-sp-C-G-A-C-G-T-C-G-T-G-G-sp-G-sp-G-sp-G[1][2].
Alimemazine D6 is deuterium labeled Alimemazine, which is an antihistamine.
VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
Compstatinis is a 13-residue cyclic peptide, and a potent inhibitor of the complement system.
cis-5-Dodecenoic acid is an endogenous metabolite with inhibitory activities against COX-I and COX-II[1].
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties[1][2][3].