Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug of Combretastatin A-1, is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 phosphate tetrasodium exhibits anti-tumor and anti-vascular effects[1][2][3].
6-O-Nicotinoylscutebarbatine G is an alkaloid that can be isolated from Scutellaria barbata.6-O-Nicotinoylscutebarbatine has cytotoxic activities against HONE-1, KB and HT29 cells with IC50s of 3.1, 2.1 and 5.7 μM, respectively[1].
Aurora Kinase Inhibitor 3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50>10 μM. Aurora Kinase Inhibitor 3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket, and several induced structural changes in the active-site compared with other published AIK structures[1].
Amphomycin is a lipopeptide antibiotic that inhibits peptidoglycan synthesis and blocks cell wall development. Amphomycin exhibits potent antibacterial activities against methicillin-resistant S. aureus (MRSA), vancomycin-resistant enterococci (VRE), penicillin-gentamicin-erythromycin-resistant S. pneumonia, and linezolid-quinupristin-dalfopristin-resistant enterococci[1][2][3].
Flumequine-13C3 is the 13C3 labeled Flumequine. Flumequine (R-802) is a quinolone antibiotic, and acts as a topoisomerase II inhibitor, with an IC50 of 15 μM (3.92 μg/mL).
NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo. IC50 value: 2.6 nMTarget: NK-1 receptorIn vitro, the binding of NKP608 to bovine retina was characterized by an IC50 of 2.6+/-0.4 nM, whereas the compound's affinity to other receptor binding sites, including NK-2 and NK-3, was much lower. Species differences in IC(50) values with NKP608 were less pronounced than with previously described NK-1 receptor antagonists, being 13+/-2 and 27+/-2 nM in gerbil midbrain and rat striatum, respectively. In vivo, using the hind foot thumping model in gerbils, NKP608 exhibited a potent NK-1 antagonistic activity following oral administration (ID(50)=0.23 mg/kg; 2 h pretreatment), supporting a central activity of NKP608. NKP608 may prove a useful anxiolytic compound.
HeE1-2Tyr, a pyridobenzothiazole compound, is a flavivirus RNA dependent RNA polymerases (RdRp) inhibitor. HeE1-2Tyr significantly inhibits West Nile, Dengue and SARS-CoV-2 RdRps (IC50 of 27.6 µM) activity in vitro[1][2].
AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus[1].
Dihydropalmatine is a alkaloid isolated from Berberis aristata[1].
FAICAR (5-Formamidoimidazole-4-carboxamide ribotide) is a purine nucleotide.
D-N-(Benzyloxycarbonyl)leucine is a leucine derivative[1].
Cycloeucalenol is a triterpenoid compound derived from Eucalyptus microcorys[1].
Scutellarin methyl ester is a constituent of Breviscapine which is a crude extract of several flavonoids of Erigeron breviscapus[1][2].
Vinaginsenoside R3 is a saponin composition of roots of Panax ginseng. Ginsengs have been not only used as therapeutic agents with tonic, sedative, anti-fatigue, and anti-gastric ulcer effect but also marketed as dietary supplements and raw materials of health food[1].
Nelonicline (ABT-126) is a selective neuronal nicotinic receptor agonist.
2-Phenylethanol-d4 is the deuterium labeled 2-Phenylethanol[1]. 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans[2]. It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
Anhydroglycinol is a phenolic compound that can be isolated from Lespedeza homoloba. Anhydroglycinol has strong antioxidative and antiallergic activity against lipid peroxidation in the rat[1].
Norepinephrine hydrochloride is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
OF-1 is a selective BRPF1B and BRPF2 bromodomain inhibitor with Kd values of 100 nM/500 nM for BRPF1B/BRPF2; 39-fold selectivity over BRD4.
S6K-18 is a potent and selective p70S6K1 inhibitor with an IC50 of 52 nM[1].
Arjunglucoside II is a triterpenes that can be isolated from Terminalia fagifolia[1].
DMT-2'-F-dA(bz) phosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.
4-Carboethoxypiperidine-d9 is the deuterium labeled 4-Carboethoxypiperidine[1].
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM[1]. WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2[2]. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively[1].
1-Phenylbutan-1-one-d5 is the deuterium labeled 1-Phenylbutan-1-one[1].
Ocedurenone is a corticosteroid receptor antagonist. Ocedurenone can be used for the research of kidney disease (WO2018054357, compound I)[1].
2-((tert-Butoxycarbonyl)amino)-2-cyclohexylacetic acid is a Glycine (HY-Y0966) derivative[1].
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K+ channels[1][2][3].
16-Acetoxy-7-O-acetylhorminone is a compound isolated from the leaves of Rabdosia lophanthoides var. gerardiana[1].
4-(3, 4-dihydroxyphenyl)butan-2-one is a compound isolated from the subspecies Lactobacillus plantarum subsp. argentoratensis. 4-(3, 4-dihydroxyphenyl)butan-2-one has antioxidant and anti-inflammatory activity. 4-(3, 4-dihydroxyphenyl)butan-2-one can be used for research of microbial fermentation [1].