Isogosferol ((+)-Isogospherol; Isogospherol) is a potent anti-inflammatory agent. Isogosferol decreases LPS (HY-D1056)-stimulated NO and IL-1β expression. Isogosferol decreases the LPS (HY-D1056)-stimulated expression of iNOS, COX-2, NF-κB, and pERK1/2[1].
COX-2-IN-26 is a potent, selective and orally active COX-2 inhibitor with IC50 values of 10.61, 0.067, 1.96 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-26 shows anti-inflammatory activity. COX-2-IN-26 shows gastrointestinal safety profile[1].
Sirtuin modulator 4 (compound 12) is a sirtuin modulator. Sirtuin modulator 4 shows inhibitory effect to SIRT1 with an EC50 value of 51-100 μM. Sirtuin modulator 4 may be used for the research of increasing the lifespan of a cell, and preventing a wide variety of diseases and disorders including, for example, diabetes, obesity, neurodegenerative diseases, cardiovascular diseases, inflammation and cancer[1].
Itch-Targeting Compound 1 is an anti-itching agent.
Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells[1]. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation[2].
ITE is a potent endogenous agonist of aryl hydrocarbon receptor (AhR), binding directly to AHR, with a Ki of 3 nM. ITE also has immunosuppressive activity.
IKK-IN-4 is a potent and selective IkappaB kinase 2 (IKKβ orIKK2) inhibitor, with IC50s of 45 and 650 nM for IKKβ and IKKα, respectively[1].
TAT-JIP inhibits the phosphorylation of endogenous c-jun activated by PHA–PMA[1].
3-O-Acetyl-α-boswellic acid suppresses T cell function[1].
TAT-MEK1 is an inhibitor ofERK2, consisting of TAT and MEK1 (N-terminal), TAT (YGRKKRRQRRR) derived from human immunodeficiency (HIV-1) transcriptional trans activator (TAT), is a cell-penetrating peptide. TAT-MEK1 IC50 in vitro for ERK2 is 29 μM[1][2].
CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells[1]. CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways[2].
Dibutyl maleate, the diester of the Maleic Acid, can be used as an intermediate of pharmaceutical synthesis. Dibutyl maleate can enhance contact sensitization to Fluorescein isothiocyanate in mice[1].
AZD8797 is an allosteric non-competitive modulator of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.
Engeletin is a flavanonol glycoside isolated from hymenaea martiana, inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
R-96544 (free base) is a potent, selective and competitive 5-HT2 receptor antagonist. R-96544 (free base) inhibits platelet aggregation induced by serotonin, and inhibits 5-HT2A receptor-mediated contraction of guinea pig trachea[1].
Thioacetamide (TAA) is an indirect hepatotoxin and causes parenchymal cell necrosis. Thioacetamide requires metabolic activation by microsomal CYP2E1 to thioacetamide-S-oxide initially and then to thioacetamide-S-dioxide, which is a highly reactive metabolite, and its reactive metabolites covalently bind to proteins and lipids thereby causing oxidative stress and centrilobular necrosis. Thioacetamide can induce chronic liver fibrosis, encephalopathy and other events model[1][2][3][4].
ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s) with an IC50 of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of ERK1/2 and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca2+-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for the treatment of inflammation related diseases[1].
Abicipar pegol (AGN-150998, MP0112) is an anti-VEGF DARPin molecule, a novel class of small proteins containing ankyrin repeat domains engineered to bind with high specificity and affinity to target proteins. Abicipar pegol effectively inhibits angiogenesis and vascular permeability and is used in the study of diseases related to ocular inflammation by intravitreal injection, reducing mean retinal thickness and leakage area[1][2].
FLAG peptide is an eight amino acids peptide (Asp-Tyr-Lys-Asp-Asp-Asp-Asp-Lys) with an enterokinase-cleavage site; designed for antibody-mediated identification and purification of recombinant proteins.
Isorabaichromone is a potent antioxidant agent. Isorabaichromone shows a potent antioxidative activity and exhibits DPPH radical and superoxide anion scavenging activities[1].
Etofenamate is a non-steroidal anti-inflammatory drug used for the treatment joint and muscular pain.
ALRN-6924 is a stapled peptide that blocks interactions between p53 and both MDM2 and MDMX[1].
Vitamin B15 (Pangamic Acid) is a natural, ubiquitously in plant seeds substance and can used be as an agent stimulating cellular respiration. Vitamin B15 contains D-gluconodimethyl amino acetic acid. Vitamin B15 is also a immune-correcting agent[1][2]. Vitamin B15 can be used for wide range of diseases.
HPK1-IN-19 is a hematopoietic progenitor kinase 1 (HPK1) inhibitor extracted from patent WO2018102366A1 compound I-47[1].
PD-1/PD-L1-IN 5 is a PD-1/PD-L1 protein/protein interaction inhibitor extracted from patent WO2017222976A1, compound Example 1, has an IC50 of ≤100 nM[1].
Decanoyl-RVKR-CMK (DecRVKRcmk) inhibits over-expressed gp160 processing and HIV-1 replication[1].
Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities[1][2][3][4][5].
c-Fms-IN-6 is a potent inhibitor of c-FMS, with an IC50 of ≤10 nM for unphosphorylated c-FMS, also weakly inhibits unphosphorylated c-KIT and PDGFR (IC50, > 1 μM). Used in the research of autoimmune diseases[1].
(-)-Zeylenol, isaolated from stems of Uvaria grandiflora, possesses anti-inflammatory and anticancer activities[1].
Itepekimab (REGN-3500; SAR-440340) is a monoclonal antibody of IL-33. Itepekimab reduces airway inflammation and related tissue damage in previous clinical studies. Itepekimab has clinical activity in asthma and has potential role in chronic obstructive pulmonary disease (COPD) and pediatric atopic dermatitis (AD)[1][2][3][4].