Koaburaside is a cytoprotective and anti-inflammatory natural compound. Koaburaside shows antioxidant activity with an IC50 of 9.0 μM for DPPH-free radical scavenging assay. Koaburaside inhibits histamine release and expressions of IL-6 and TNF-α in human mast cells. Koaburaside also effectively inhibits influenza A neuraminidase[1].
CP19, a histamine receptor antagonist, is an entry inhibitor against both Ebolavirus (EBOV) and Marburgvirus (MARV) with IC50s of 3.4 μM and 29.5 μM, respectively. CP19 has SI values of 29.4 and 3.4 for EBOV and MARV, respectively. CP19 has antiviral activity[1].
Ibuprofen impurity 1 is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[1].
Cetirizine methyl ester is an impurity of Cetirizine (HY-17042). Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist[1].
3-O-(2'E,4'Z-Decadienoyl)ingenol is a natural diterpene that exhibits significant anticomplement activity with an IC50 of 89.5 μM[1].
Gilvetmab is a potent caninized antiPD-1 monoclonal antibody. gilvetmab blocks the interaction between PD-1 and its ligand PDL-1[1].
CB-1158 is a potent and orally bioavailable inhibitor of arginase, with IC50s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively.
GP130 receptor agonist-1 is a potent, brain-penetrant and orally active GP130 receptor agonist. GP130 receptor agonist-1 has a neuroprotective effect on NMDA-induced neurotoxicity[1].
Robinin is present in flavonoid fraction of Vigna unguiculata leaf. Robinin inhibits upregulated expression of TLR2 and TLR4. Robinin ameliorates oxidized low density lipoprotein (Ox-LDL) induced inflammatory insult through TLR4/NF-κB pathway[1].
Factor B-IN-3 (Example 3 target compound) is a potent complement factor B inhibitor. Factor B-IN-3 can be used for the research of diseases related to inflammation and immunity[1].
Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth[1][2].
Apilimod is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively.
Isofezolac (LM 22070) is a non-steroidal anti-inflammatory drug (NSAID) that inhibits prostaglandin-synthetase. Isofezolac anti-inflammatory, and antipyretic properties[1][2].
1400W dihydrochloride is a potent and selective inhibitor of human inducible NO synthase with Ki values of 7 nM.
Pectolinarin, isolated from Cirsium chanroenicum, possesses anti-inflammatory activity[1]. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin suppresses cell proliferation and inflammatory response and induces apoptosis via inactivation of the PI3K/Akt pathway[2].
Eritoran is a Toll-like receptor 4 (TLR4) antagonist. Eritoran protects mice against lethal influenza virus infection, such as Ebola virus (EBOV), Marburg virus (MARV). Eritoran decreases the level of granulocytosis, may alleviate the severity of the "cytokine storm". Eritoran inhibits pathogenesis of filovirus infection[1].
Triptoquinone B ((+)-Triptoquinone B), a sesquiterpene alkaloid, is an interleukin-1 inhibitor. Triptoquinone B shows potent inhibitory activities against interleukin 1α and β releases for human peripheral mononuclear cells[1][2].
Pimivalimab (JTX-4014) is a PD-1 inhibitor. Pimivalimab can be used for the research of solid tumor[1].
Adebrelimab (SHR-1316) is a humanized IgG4 monoclonal PD-L1 (PD-1/PD-L1) antibody. Adebrelimab has promising antitumor activity in solid tumors including extensive-stage small-cell lung cancer (SCLC)[1][2].
FD-IN-1 (Compound 12) is a factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5µM, respectively[1].
C3a (70-77) is an octapeptide corresponding to the COOH terminus of C3a, exhibits the specificity and 1 to 2% biologic activities of C3a.
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.)[1]. Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects[2]. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM[3].
ST-1006 maleate is a potent histamine H4 receptor agonist with a pKi value of 7.94. ST-1006 maleate has anti-inflammatory effect[1][2].
Tildrakizumab (SCH 900222) is a humanized anti-IL-23 (p19 subunit) monoclonal antibody. IL-23 is a critical cytokine to maintain the Th17 cell phenotype. Tildrakizumab has high-affinity for single-chain IL-23 (Kd: 136 pM). Tildrakizumab is effective against moderate to severe plaque psoriasis[1][2][3].
CAY 10465 is a selective and high-affinity AhR agonist, with a Ki of 0.2 nM, and shows no effect on estrogen receptor (Ki >100000 nM).
CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator with an EC50 value of 100 nM. CXCR4 modulator-1 can be used for researching anti-inflammatory, anticancer and anti-HIV[1].
Meclizine D8 (Meclozine D8) is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR[1][2][3].
Etoricoxib-d3 is the deuterium labeled Etoricoxib[1]. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood[2][3][4].
Imiquimod maleate is an immune response modifier that acts as a toll-like receptor 7agonist.
Naphazoline (Naphthazoline) nitrate is an α-adrenergic receptor agonist. Naphazoline nitrate reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline nitrate reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline nitrate can be used for non-bacterial conjunctivitis research[1][2].