ICI 211965 is a selective and orally potent 5-Lipoxygenase (5-LPO) inhibitor.
Plerixafor is a selective CXCR4 antagonist with an IC50 of 44 nM.
Pirfenidone is a drug used for the treatment of idiopathic pulmonary fibrosis. It inhibits FGFR, EGFR, PDGFR, TGF-β, thereby slowing tumor cell proliferation.
Ketorolac D5 is a deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2[1].
Norathyriol (Mangiferitin) is a natural metabolite of Mangifera. Norathyriol inhibits α-glucosidase in a noncompetitive manner with an IC50 of 3.12 μM[1]. Norathyriol inhibits PPARα, PPARβ, and PPARγ with IC50s of 92.8 µM, 102.4 µM, and 153.5 µM, respectively[2]. Antioxidant, anticancer, antimicrobial, anti-inflammatory, anti-bacterial activities.
Ermanin is a flavonoid isolated from Tanacetum microphyllum. Ermanin potently inhibits iNOS, COX-2 activities, and inhibits platelet aggregation. Ermanin has anti-inflammatory, anti-tuberculous and anti-viral/bacterial properties[1][2].
URAT1 inhibitor 6 (Compound 1h) is a potent URAT1 inhibitor (IC50: 35 nM for hURAT1). URAT1 inhibitor 6 is 200- and 8-fold more potent than parent Lesinurad (HY-15258) and Benzbromarone (HY-B1135). URAT1 inhibitor 6 can be used for research of inflammation[1].
NS-3-008 is a novel small-molecule transcriptional inhibitor of G0s2 (G0/G1 switch 2) with IC50 of 2.25 uM; decreases levels of G0s2 and Ccl2 mRNA in the kidneys (5 mg/kg, p.o.); decreases the phosphorylation of Stat5 and p65 protein and suppresses renal inflammation in 5/6Nx mice, ameliorates renal dysfunction in mouse model of chronic kidney disease (CKD).
Rosiglitazone (BRL49653) is a potent thiazolidinedione insulin sensitizer. Rosiglitazone is a selective PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively.
Calf thymus DNA is high quality double-stranded template DNA isolated from the thymus of male and female calves.
RIPK1-IN-9 (example 45), a dihydronaphthyridone compound, is a potent and selective RIPK1 inhibitor. RIPK1-IN-9 inhibits U937 cell (IC50=2 nM) and L929 cell (IC50=1.3 nM)[1].
MMI-0100 is a cell-permeant peptide inhibitor of mitogen activated protein kinase activated protein kinase II (MK2). MMI-0100 reduces intimal hyperplasia ex vivo and in vivo. MMI-0100 suppresses IL-6 expression without effect on IL-8 expression. MMI-0100 suppresses fibrotic processes such as vein graft disease[1].
Tau-aggregation and neuroinflammation-IN-1 is a potent tau-aggregation and neuroinflammation inhibitor. Tau-aggregation and neuroinflammation-IN-1 exhibits remarkable inhibitory activities against AcPHF6 and full-length tau aggregation. Tau-aggregation and neuroinflammation-IN-1 has a low cytotoxicity and reduced NO release in LPS-stimulated BV2 cells. Tau-aggregation and neuroinflammation-IN-1 can reverse okadaic acid-induced memory impairment in rats[1].
Odulimomab (anti-LFA1) is an anti-LFA-1 monoclonal antibody. Odulimomab inhibits proliferation of T lymphocyte and shows protective effects against ischemia and reperfusion injury. Odulimomab can be used for the research of transplant rejection and immunological disease[1][2].
Tricarbonyldichlororuthenium(II) dimer is a pharmacological donor of CO releasing. CO releases from Tricarbonyldichlororuthenium(II) dimer prevents gastric mucosal oxidative damage induced by ischemia/reperfusion (I/R) improving gastric blood flow (GBF), decreasing DNA oxidation and inflammatory response on systemic level[1].
WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122 ± 30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells.
Dexamethasone acetate is a glucocorticoid receptor agonist.
6-O-Methyl Guanosine is a modified nucleoside[1]. 6-O-Methyl Guanosine (6-methylguanosine) inhibit colony-forming ability in a malignant xeroderma pigmentosum cell line[2].
Piperundecalidine is an amide alkaloids that can be purified from Piper longum L. Piperundecalidine shows various biological properties, such as anti-inammatory, analgesic, anti-amoebic, anti-depressant, hepatoprotective,etc.[1].
Keap1-Nrf2-IN-12 is a potent Keap1-Nrf2 inhibitor with an IC50 value of 2.30 µM. Keap1-Nrf2-IN-12 shows metabolic stability in human liver microsomes[1].
Frentizole, an FDA-approved immunosuppressive drug, is a novel inhibitor of the Aβ-ABAD interaction.IC50 value:Target: Aβ-ABAD interaction
Lup-20(29)-en-28-oic acid, a triterpenoid saponins of Pulsatilla koreana Root, possesses anti-inflammatory and anti-tumor effect[1][2].
Lirimilast (BAY 19-8004) is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 value of 49 nM. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease (COPD). Lirimilast has potently anti-inflammatory properties[1][2].
ThioLox is a competitive 15-lipoxygenase-1 (15-LOX-1) inhibitor with a Ki of 3.30 μM. ThioLox shows anti-inflammatory and neuroprotective properties[1].
GSK-5498A is a selective small molecule blocker of CRAC channel(IC50=1 uM); inhibit mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.IC50 value: 1 uM [1]Target: CARC channel blocker GSK-5498A completely inhibited calcium influx through CRAC channels. This led to inhibition of the release of mast cell mediators and T-cell cytokines from multiple human and rat preparations. Mast cells from guinea-pig and mouse preparations were not inhibited by GSK-5498A.
AX-024 hydrochloride is an cytokine release inhibitor which can strongly inhibit the production of interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10 and IL-17A.
Pyrisoxazole (SYP-Z048) is a fungicide[1].
Saralasin ([Sar1,Ala8] Angiotensin II) acetate hydrate is an octapeptide analog of angiotensin II. Saralasin acetate hydrate is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin acetate hydrate can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension[1][3][6].
(-)-Pinoresinol is a plant-derived tetrahydrofuran lignan that inhibits α-glucosidase and acts as a hypoglycemic agent. (-)-Pinoresinol has some anti-inflammatory effects and acts as a chemopreventive agent, inducing increased apoptosis and cell cycle G2/M arrest[1].
Resorcinol is an antiseptic and a disinfectant, and a chemical intermediate for the production of many other pharmaceuticals，is used to treat acne, seborrheic dermatitis, eczema, psoriasis, and other skin disorders.