4-CPPC is the first reversible and selective inhibitor of pro-inflammatory protein macrophage migration inhibitory factor-2 (MIF-2) with Ki of 33 uM, 13-fold selectivity for human MIF-2 versus human MIF-1.
κ-Carrageenan is a natural polymer which predominantly available in red seaweeds. κ-Carrageenan is an effective drug carrier to deliver curcumin in cancer cells and to induce apoptosis. κ-carrageenan serves as a potential inflammatory agent that magnifies existing intestinal inflammation[1][2].
Allosecurinine (Phyllochrysine) is a Securinega alkaloid isolated from M.indica and M.discoidea[1].
Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects[1][2].
Tr-PEG4-OH is a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
Streptazolin is an antibiotic. Streptazolin increases bacterial killing and elaboration of immunostimulatory cytokines by macrophages in vitro. Streptazolin stimulates the macrophage NF-κB pathway via PI3K signaling[1][2].
BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively[1][2].
JAK-IN-24 is a JAK inhibitor, with IC50s of 0.534 and 24 nM at the presence of 4 μM or 1mM ATP, respectively. JAK-IN-24 also inhibits PBMC IL-15 induced STAT5 phosphorylation with an IC50 of 86.171 nM[1].
SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor.
Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
C87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
Atrazine-3-mercaptopropanoic acid is a hapten. The IC50 value of polyclonal antibody (PcAb) 1 with coating Atrazine-3-mercaptopropanoic acid is 7.5 ng/mL[1].
KAT8-IN-1 is a lysine (K) acetyltransferase 8 (KAT8) inhibitor, with IC50s of 141 μM (KAT8), 221 μM (KAT2B), 106 μM (KAT3B), respectively. KAT8 inhibits histone acetyltransferases (HATs), and could result in disease states, such as cancer or inflammatory diseases[1].
4-Hydroxy Atorvastatin lactone is a metabolite of Atorvastatin (HY-B0589). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids[1].
Darbufelone mesylate is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
Plaunotol is an orally active acyclic diterpene alcohol. Plaunotol has antibacterial activity against Helicobacter pylori which causes peptic ulcer [1]. Plaunotol inhibits tumor angiogenesis and cell proliferation. Plaunotol induces apoptosis by activation of caspase 8 and caspase 9 pathways. Plaunotol is a potential anticancer agent against colon cancer [2].
PF-3893787 hydrochloride is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4 nM) and is also a functional (Ki=1.56 nM) antagonist.
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro[1][2][3].
Hydroxyzine-d8 Dihydrochloride is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder[1][2].
Cevidoplenib is a potent, selective Syk kinase inhibitor for treatment of kinase-mediated diseases.
2-(Phosphonooxy)benzoic acid is a non-acetylated salicylic acid derivative which is used for treating inflammatory disease as well as in analgesic therapy[1].
17-Hydroxyneomatrine, extracted from Sophora flavescens, can well inhibit the growth of human cervical carcinoma Hela cells, has the wide-range antibacterial, anti-allergy, anti-tumor, anti-arrhythmia, swelling-subsiding diuresis, immunizing, and biological regulation functions[1].
TR-14035 is a a dual alpha4beta7(IC50=7 nM)/alpha4beta1 (IC50=87 nM) integrin antagonist .IC50 Value: alpha(4)beta(7)/alpha(4)beta(1)=7/87 nM [1]Target: integrinTR14035 blocked the binding of human alpha(4)beta(7) to an (125)I-MAdCAM-Ig fusion protein with IC(50) values of 0.75 nM. TR14035 blocked binding of human alpha(4)beta(7)-expressing RPMI-8866 cells or murine mesenteric lymph node lymphocytes to MAdCAM-Ig with IC(50) values of 0.1 microM [2]. TR14035 blocked adhesion to HEVs [ED(50) of 0.01-0.1 mpk i.v.].TR-14035 was taken up by rat and human hepatocytes by an apparently single saturable mechanism with K(m) of 6.7 and 2.1 microM, respectively, and taurocholate and digoxin reduced this uptake [3].
Mesaconinean, an ingredient from Aconitum carmichaelii Debx., has cardiac effect[1].
2-(N-Phthalimidoylmethylthio)acetic acid (MFA) is a hapten with a carboxyl group at the end of its spacer arm, suitable for reacting with free amine groups of proteins. 2-(N-Phthalimidoylmethylthio)acetic acid can be combined with carrier proteins and used in antigen design[1].
PAT-1251 Hydrochloride is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively).
NLRP3-IN-15 is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-15 inhibits IL-1β release with an IC50 of 0.114 μM. NLRP3-IN-15 can be used for the research of inflammation[1].
SCD1-IN-1 is a SCD1 inhibitor (IC50: 5.8 nM). SCD1-IN-1 can be used in the research of dermatologic condition[1].
Tosufloxacin (tosylate hydrate) is a fluoroquinolone antibacterial agent. Tosufloxacin (tosylate hydrate) is effective against Gram-positive and Gram-negative aerobic bacteria, anaerobic bacteria and Chlamydia trachomatis. Tosufloxacin (tosylate hydrate) is also a bacterial Topo (DNA gyrase, topoisomerase)) inhibitor.
Chitopentaose pentahydrochloride is a chitosan oligosaccharide with anti-inflammatory effect. Chitopentaose pentahydrochloride is a substrate of gene encoding chitinase B (FjchiB)[1][2].