A dual inhibitor of E selectin and CXCR4 with IC50 of 3.6 uM and 1.1 uM respectively, blocks adhesion of AML blasts to E-Selectin, mobilizes human AML engrafted in mice.

A dual inhibitor of E selectin and CXCR4 with IC50 of 4.1 uM and 30 nM respectively, blocks adhesion of AML blasts to E-Selectin, mobilizes human AML engrafted in mice.

Gingerenone A is a Nrf2-Gpx4 activator with anti-breast-cancer properties. Gingerenone A results a delayed G2/M in cancer cells, following oxidative stress and senescence responses. Gingerenone A also alleviates ferroptosis in secondary liver injury (SLI) in dextran sodium sulfate (DSS)-induced colitis mice. Gingerenone A can be isolated from Zingiber officinale.

A dual inhibitor of TNF-α and TGF-β1 by inhibiting IκB kinase phosphorylation and Smad3 phosphorylation.

Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.IC50 value: 1.3/0.7 nM(OX1/OX2 receptor) [1] [2]Target: Dual OX!/OX2 receptorin vitro: [(3)H]Almorexant bound to a single saturable site on hOX(1) and hOX(2) with high affinity (K(d) of 1.3 and 0.17 nM, respectively. In Schild analyses using the [(3)H]inositol phosphates assay, almorexant acted as a competitive antagonist at hOX(1) and as a noncompetitive-like antagonist at hOX(2). In binding kinetic analyses, [(3)H]almorexant had fast association and dissociation rates at hOX(1), whereas it had a fast association rate and a remarkably slow dissociation rate at hOX(2) [1]. in vivo: During the 12-h dark period after dosing, ALM(Almorexant) exacerbated cataplexy in TG mice and increased nonrapid eye movement sleep with heightened sleep/wake fragmentation in both genotypes. ALM showed greater hypnotic potency in WT mice than in TG mice. The 100 mg/kg dose conferred maximal promotion of cataplexy in TG mice and maximal promotion of REM sleep in WT mice. In TG mice, ALM (30 mg/ kg) paradoxically induced a transient increase in active wakefulness [3]. Almorexant 200 mg showed significantly less 'Drug Liking' than both zolpidem doses (p < 0.01), and almorexant 400 mg had smaller effects than zolpidem 20 mg (p < 0.05), while almorexant 1,000 mg was not different from either zolpidem dose [4].

trans-ACPD is a selective agonist for metabotropic glutamate receptors, acting at both group I and group II mGlu receptors.

A first-generation antihistamine that acts primarily as H1 receptor antagonist.

A first-in-class analogue of unacylated ghrelin, and unacylated ghrelin receptor agonist.

A first-in-class antitumor and antimetastatic agent that induces necrosis in breast cancer tumors, inhibits inhibit mitochondria complex I activity and reduces HIF-1α stabilization.

A first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM).

A first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM).

A first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM).

A first-in-class, selective, orally bioavailable, dual inhibitor of BTK and PI3Kδ kinases with IC50 of 32.3 nM and 16.9 nM, respectively.

A first-in-class, small molecule protein-protein inhibitor of the interaction between the E1 and E2 proteins of HPV types 6 and 11.

A form of dynorphin and an endogenous opioid peptide with the amino acid sequence: Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys..

A fourth-generation fluoroquinolone antibiotic that inhibits the bacterial DNA gyrase and topoisomerase IV.

A fourth-generation fluoroquinolone antibiotic that inhibits the bacterial DNA gyrase and topoisomerase IV.

A fourth-generation fluoroquinolone antibiotic that inhibits the bacterial DNA gyrase and topoisomerase IV.

A fourth-generation synthetic fluoroquinolone, broad-spectrum antibacterial agent that is active against both Gram-positive and Gram-negative bacteria.

A fucose analog that inhibits Dll-induced Notch signaling by reducing Notch ligand Dll1-Notch1 binding, but not Jag1.

A fungal natural product that binds to HuR and inhibits HuR-RNA interaction in vitro with IC50 of 1.2 uM.

A GABA receptor agonist and modulator of glutamatergic systems.