punicalagin is a major ellagitannin found in pomegranates that is reported to produce antioxidant, anti-inflammatory, and anticancer effects. it has been shown to prevent high-fat diet-induced obesity-associated accumulation of cardiac triglyceride and ch
sirt7 inhibitor 97491 is an hdac inhibitor with high specificity for sirt7 (ic50 = 325 nm). sirt7 inhibitor 97491 promotes apoptosis through caspase pathway.
astragaloside ii is an effective mdr reversal agent and may be a potential adjunctive agent for hepatic cancer chemotherapy. astragaloside ii also induces osteogenic activities, differentiation, proliferation, and mineralization, through the bone morphoge
echinatin disturb the mitochondrial energy transfer reactions and membrane permeability, at a low concentration cause deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria, inhibits dnp-atpase activity while
phellopterin is a partial agonist of the central benzodiazepine receptors in vitro. phellopterin shows a cytotoxic effect on raw264.7 cell at the concentration from 40 to 400 μm. phellopterin reduce tnf-alpha-induced vcam-1 expression through regulation o
befotertinib (d-0316) is the third-generation egfr tyrosine kinase inhibitor. befotertinib can be used for the research of egfr t790m-positive non-small cell lung cancer (nsclc).
est73502 is an agonist of μ-opioid receptor(ki = 64 nm) agonist and an antagonist of σ1 receptor (ki = 118 nm). est73502 displays antinociceptive activity.
kaurenoic acid has anti-inflammatory potential in acetic acid-induced colitis, decreases in mda level. kaurenoic acid exerts a uterine relaxant effect acting principally through calcium blockade and in part, by the opening of atp-sensitive potassium chann
boc-asp(ome)-fluoromethyl ketone is a broad range caspase inhibitor that inhibits fas-mediated phagocytosis and oxidative rupture inhibition, but does not affect the chemotactic activity of il-8 [1] [2] .
jatrorrhizine is a protoberberine alkaloid isolated from enantia chlorantha (annonaceae) and other species. it was found to have antimicrobial and antifungal activity. it binds and noncompetitively inhibits monoamine oxidase (ic50 4 micromolar for mao-a a
isavuconazonium sulfate is hydrolyzed by plasma esterases to yield the active moiety isavuconazole. isavuconazole binds to and inhibits the fungal cytochrome p450 family enzyme lanosterol 14-alpha-demethylase (cyp51), which catalyzes the demethylation of
c-type natriuretic peptide (cnp) (1-22), human acetate is an agonist of natriuretic peptide receptor b (npr-b), an endothelial-derived relaxant and growth inhibitory factor. c-type natriuretic peptide (cnp) (1-22), human acetate inhibits camp synthesis s
cid5721353 is a b-cell lymphoma 6 inhibitor (bcl6 inhibitor) that disrupts bcl6/corepressor complexes in vitro and in vivo, and was shown to bind the critical site within the btb groove.
choline fenofibrate is a choline formulation of fenofibrate, a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity.
radiprodil (rgh-896) is an orally active and selective nmda nr2b receptors antagonist. it was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (dpnp).
asapiprant (s-555739) is a potent and selective dp1 receptor antagonist (ki: 0.44 nm). it exhibited high affinity and selectivity for the dp1 receptor.
volinanserin (mdl 100907) is a potent and selective antagonist of the serotonin receptor 5-ht2 (ki: 0.36 nm) and shows 300-fold selectivity for 5-ht2 receptor over 5-ht1c, alpha-1 adrenergic and sigma receptors.
ck1-in-1, compound 1c reported in patent wo2015119579a1, is a casein kinase 1 (ck1) inhibitor. it has ic50s of 15 nm, 16 nm, 73 nm for ck1δ, and ck1ε, p38σ mapk, respectively.
prulifloxacin is a broad-spectrum fluoroquinolone antibiotic. it inhibits bacterial dna synthesis by inhibiting the activity of bacterial dna topoisomerase ii and iv.
bms-599626 (ac480) is a selective inhibitor of her1 and her2 (ic50s: 20 nm and 30 nm), ~8-fold less potent to her4, >100-fold to lck, vegfr2, c-kit, met, etc.
ddd107498 has a potent and novel spectrum of antimalarial activity against multiple life-cycle stages of the plasmodium parasite. it targets translation elongation factor 2 (eef2).
bms986195 is a potent, covalent inhibitor of bruton´s tyrosine kinase (btk), >5,000-fold selective over all kinases outside of the tec family (ic50 <1 nm for btk).
bi-3802 is a highly potent bcl6 degrader and inhibits the bric-à-brac (btb) domain of bcl6 with an ic50 value of ≤3 nm. bi-3802 induces the polymerization of bcl6 and promotes bcl6 degration depended on e3 ligase siah1. bi-3802 has antitumor activity[1][2
azd3229 is a potent pan-kit mutant inhibitor for the treatment of gastrointestinal stromal tumors. it demonstrates potent single-digit nm growth inhibition across a broad cell panel.
pd 158780 reversibly inhibits auto and transphosphorylation of all four members of the erbb receptor superfamily: egfr, erbb2, erbb3, and erbb4 (ic50s: 8μm, 49 nm, 52 nm, and 52 nm in cell assay).