Isomucronulatol 7-O-glucoside is a flavonoid isolated from the roots of A. membranaceus. Isomucronulatol 7-O-glucoside exhibits weak inhibitory effects on LPS-stimulated production IL-12 p40 in vitro and has potential anti-inflammatory effect[1].
Endothelin 1 (swine, human) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 acts through two types of receptors ETA and ETB.
Schisandrin has various therapeutic effects on a range of medical conditions such as anti-asthmatic, anti-cancer, and anti-inflammatory effects.IC50 value:Target:in vitro: Sch inhibited the pro-fibrotic activity of TGF-β1 in AML12 cells; thus, it suppressed the accumulation of ECM proteins. Also, Sch inhibited the EMT as assessed by reduced expression of vimentin and fibronectin, and increased E-cadherin and ZO-1 in TGF-β1 induced AML12 cells. Sch reduced TGF-β1-mediated phosphorylation of Smad2/3 and Smad3/4 DNA binding activity. On the other hand, Sch reduced TGF-β1-induced ERK1/2 and PI3K/Akt phosphorylation in the non-Smad pathway [1]. the anti-inflammatory properties of schisandrin result from the inhibition of nitric oxide (NO) production, prostaglandin E(2) (PGE(2)) release, cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) expression, which in turn results from the inhibition of nuclear factor-kappaB (NF-kappaB), c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase (MAPK) activities in a RAW 264.7 macrophage cell line [2].
Z62954982 is a potent, specific Rac1 inhibitor, reduces the intracellular levels of Rac1-GTP in a concentration-dependent manner with IC50 of 12 uM, 4 times more effective than NSC23766 (IC50=50 uM); causes a concentration-dependent decrease in transendothelial electrical resistance (TER) in both HDMEC and HUVEC.
Tpl2 Kinase Inhibitor 1 (Compound 1) is a potent and selective Tpl2 (COT kinase, MAP3K8) inhibitor, plays an important role in the regulation of the inflammatory response and the progression of some cancers[1].
LY 292728 is a potent leukotriene B4 (LTB4) receptor antagonist. LY 292728 binds to human neutrophils with a Ki of 0.47 nM and binds to guinea pig lung membranes with a Ki of 0.04 nM[1].
BMS-986142 is a potent and highly selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.5 nM.
diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist.
Histatin 5 inhibits the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively.
YM-264 is a selective, potent and orally active platelet-activating factor (PAF) antagonist with a pKi value of 8.85 for rabbit platelet membranes.
Lampalizumab (RG 7417) is a humanised monoclonal antibody targeting complement Factor D in the alternative complement pathway. Lampalizumab binds an exosite and sterically blocks Factor B access to the active site. Lampalizumab can be used for age-related macular degeneration (AMD) research[1][2].
Nicotredole (Tryptamide) is an orally active anti-inflammatory and analgesic agent. Nicotredole exhibits evident antiinflammatory effects of potency comparable with Phenylbutazone. Nicotredole has only weak ulcerogenic activity[1][2][3].
Robustine, a furoquinoline alkaloid, from Dictamnus albus, exhibits inhibitory potency against human phosphodiesterase 5 (hPDE5A) in vitro[1].
IGF-I (30-41) is amino acids 30 to 41 fragment of Insulin-like Growth Factor I (IGF-I). IGF-I is partly responsible for systemic GH activities although it possesses a wide number of own properties (anabolic, antioxidant, anti-inflammatory and cytoprotective actions)[1].
Chlorcyclizine hydrochloride is a histamine H1 antagonist.
BMS-935177 is a potent and selective reversible inhibitor of Bruton’s tyrosine kinase (Btk) with an IC50 of 3 nM.
Salicylic acid inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation.
6(5H)-Phenanthridinone is a potent PARP-1 inhibitor and immunomodulator. 6(5H)-Phenanthridinone inhibits cell proliferation and can be used in cancer research[1].
Andrographolide (Andro) is a small antagonist for NF-κB activation by covalent modifying reduced cysteine 62 of p50. Andrographolide is a bicyclic diterpenoid lactone mainly produced from the plant Andrographis (Andrographis paniculate).Andrographolide suppresses the activation of NF-κB in stimulated endothelial cells, which reduces the expression of cell adhesion molecule E-selectin and prevents E-selectin-mediated leukocyte adhesion, but has no effect on IκBα degradation, p50 and p65 nuclear translocation[1].
10-Hydroxyaloin B is a bioactive oxanthrone based on the aloin skeleton[1].
Ecliptasaponin D is a triterpenoid glucoside isolated from Eclipta alba (L.) Hassk which is the aerial part of Eclipta prostrate. Eclipta prostrate is considered as a nourishing herbal medicine with pleiotropic effects, including anti-inflammatory, hepatoprotective, antioxidant and immunomodulatory[1,2].
Rupatadine D4 fumarate (UR-12592 D4 fumarate) is a deuterium labeled Rupatadine fumarate. Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 μM(rabbit platelet membranes/guinea pig cerebellum membranes)[1][2][3].
Nadifloxacin(OPC7251) is a topical fluoroquinolone antibiotic for the treatment of acne vulgaris. Target: AntibacterialNadifloxacin is a potent, broad-spectrum, quinolone agent approved for topical use in acne vulgaris and skin infections. Nadifloxacin inhibits the enzyme DNA gyrase that is involved in bacterial DNA synthesis and replication, thus inhibiting the bacterial multiplication. In vitro studies of nadifloxacin show potent and broad-spectrum antibacterial activity against aerobic Gram-positive, Gram-negative and anaerobic bacteria. Additionally, studies also suggest that the effectiveness of nadifloxacin in inflammatory acne lesions may be attributed to its inhibitory effect on pro-inflammatory cytokines like interleukin (IL)-1α, IL-6, and IL-8 which also play an important role in acne pathogenesis [1, 2].
Larazotideis a peptide which is an orally active zonulin antagonist. Larazotide shows antiviral activity to varicella-zoster virus (VZV) with EC50s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide can be used for the research of celiac disease and infection[1][2].
Usaramine N-oxide, a flavonoid isolated from Crotalaria pallida, possesses anti-inflammatory activities[1].
SC-26196 is a potent, orally active Delta6 desaturase (D6D) inhibitor (IC50=0.2 µM in a rat liver microsomal assay). Antiinflammatory properties[1].
Kumujian A (1-Ethoxycarbonyl-β-carboline), an anti-inflammatory agent, inhibits both superoxide anion generation (IC50 = 4.87 μg/mL) and elastase release (IC50 = 6.29 μg/mL)[1].
MSC2360844 is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 shows highly selective against a panel of 278 additional kinases[1].
Ezurpimtrostat hydrochloride (compound 2-3) is a potent and orally active anti-fibrotic agent. Ezurpimtrostat hydrochloride reduces significantly the liver fibrosis in DEN (diethyl nitrosamine) cirrhotic rat model. Ezurpimtrostat hydrochloride can be used for the research of fibrosis, cancer, autophagy and cathepsins B (CTSB), L (CTSL) and D (CTSD) related diseases [1].
MrgprX2 antagonist-2 is an MrgprX2 antagonist extracted from patent WO2021092262A1, example E163. MrgprX2 antagonist-2 can be used for the research of inflammatory disorders of the skin[1].