A derivative of EDTA that chelates iron and reduces the number of metal ions complexed with anthracycline and, consequently, decrease the formation of superoxide radicals.

A derivative of the neurotransmitter GABA that acts as a GABAB receptor agonist.

A des acryl analogue of AZD9291 that is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant..

A drug-linker conjugate for Antibody-drug conjugates (ADCs) by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the cleavable peptide Val-Cit-PAB..

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.

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

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

A glycolytic inhibitor that inhibits hexokinase II activity, suppresses ATP production, and induces endoplasmic reticulum (ER) stress.

A growth hormone-release inhibiting factor used in the treatment of severe, acute hemorrhages of gastroduodenal ulcers.

A guanosine analogue antiviral agent used for the treatment of various herpesvirus (HSV) infections.

SPDP (SPDP Crosslinker) is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls. It is a glutathione cleavable ADC linker u

PD 404182 is a high affinity inhibitor of KDO 8-P synthase (Ki = 26 nM). Also inhibits dimethylarginine dimethylaminohydrolase 1 (DDAH1). Exhibits antiangiogenic and antiviral activity in vitro. Putative antibiotic against gram-negative bacteria.

A highly potent agonist of σ1 receptor with Ki of 0.8 nM.

A highly potent and selective inhibitor of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.

A highly potent sigma receptor agonist with Ki of 1.7 nM and 25.2 nM for σ1 and σ2, respectively.

A highly potent, orally bioavailable, pan-VEGFR inibitor with IC50 of 1, 5, 3 nM for VEGFR1, 2, 3, respectively.

A highly potent, selective and orally bioavailable trace amine-associated receptor 1 (TRRA1) full agonist with EC50 of 18 nM, >500-fold selectivity over human adrenergic α2A receptor.

A highly potent, subtype-selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 17 nM, without inhibitory activity for MCHR2 at 10 uM.

A highly selective, non-ATP competitive substrate-pocket-directed Src/pretubulin inhibitor.

A highly selective, non-ATP competitive substrate-pocket-directed Src/pretubulin inhibitor.