Neuropeptide Y (13-36), porcine is a selective neuropeptide Y2 receptor agonist[1].
Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor[1].
(Des-Gly2)-Exenatide is a potential impurity of Exenatide (HY-13443).
2,3',4,6-Tetrahydroxybenzophenone, a kind of benzophenone, is the immediate precursor of xanthones in higher plants[1].
2,3,5,6,7,8-Hexahydro-1H-cyclopenta[b]quinolin-9-amine is a pharmaceutically active compound which is a nootropic agent that acts as cholinesterase inhibitor and is used in treatment of Alzheimer disease[1].
Valiolamine, an aminocyclitol has been isolated from the fermentation broth of Streptomyces hygroscopicus subsp. Valiolamine has potent alpha-glucosidase inhibitory activity against porcine intestinal sucrase, maltase and isomaltase[1].
MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor with an IC50 value of 81.0 nM. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1. MCT1-IN-3 can be used for the research of cancer[1].
Neuraminidase-IN-8 (Compound 6d) is a potent neuraminidase inhibitor with an IC50 of 0.027 µM. Neuraminidase-IN-8 shows anti-influenza activities[1].
DL-Leucyl-DL-phenylalanine is a dipeptide and can be used as a substrate to detecte two regions of dipeptidase staining on a gel in Drosophila simulans as well as in Drosophila melanogaster[1][2].
MGAT2-IN-1 is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.
HAEGT is the first N-terminal 1-5 residues of GLP-1 peptide.
AZ7550-d5 is the deuterium labeled AZ7550 (HY-B0794). AZ7550, an active metabolite of AZD9291 (HY-15772), inhibits the activity of IGF1R with an IC50 of 1.6 μM[1][2].
5’-Deoxy-5’-(4-morpholinyl)thymidine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
ML344 is a CqsS/LuxQ agonist probe that acts as an inducer of light production without autoinducers.
Rocaglamide is a potent NF-κB activation inhibitor.
SARS-CoV-2-IN-68 (compound 6C) is a covalent SARS-CoV-2 PLpro/Mpro inhibitor with potent antiviral activities. SARS-CoV-2-IN-68 binds to Zn-finger domain of PLpro[1].
Brompheniramine maleate is a histamine H1 receptors antagonist.Target: Histamine H1 ReceptorBrompheniramine maleate, is an antihistamine drug of the propylamine (alkylamine) class. It is readily available over the counter and is indicated for the treatment of the symptoms of the common cold and allergic rhinitis. It is a first-generation antihistamine. Brompheniramine has antidepressant properties, inhibiting reuptake of the neurotransmitter serotonin. Based on this knowledge, Arvid Carlsson and his colleagues, working at the Swedish company Astra AB, were able to derive the first marketed selective serotonin reuptake inhibitor, zimelidine, from brompheniramine. Brompheniramine had a long half-life and large volume of distribution in normal adults. It also had a prolonged antihistaminic effect in the skin as evidenced by suppression of the wheal and flare response to histamine and by suppression of pruritus [1, 2].
NPS-2143(SB 262470A ) is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively.IC50 value: 43 nM(for Ca2+ receptor) [1]Target: CaSRin vitro: NPS 2143, even when tested at much higher concentrations (3 microM), did not affect the activity of a number of other G protein-coupled receptors, including those most structurally homologous to the Ca2+ receptor. NPS 2143 stimulated parathyroid hormone (PTH) secretion from bovine parathyroid cells (EC50 of 41 nM) over a range of extracellular Ca2+ concentrations and reversed the effects of the calcimimetic compound NPS R-467 on [Ca2+]i and on secretion of PTH [1]. The first reported calcilytic compound was NPS 2143, an orally active molecule which elicits rapid, 3- to 4-fold increases in circulating levels of PTH [2].in vivo: When infused intravenously in normal rats, NPS 2143 caused a rapid and large increase in plasma levels of PTH. Ca2+ receptor antagonists are termed calcilytics and NPS 2143 is the first substance (either atomic or molecular) shown to possess such activity [1]. When administered together with an antiresorptive agent (estradiol), NPS 2143 causes an increase in trabecular bone volume and bone mineral density in osteopenic rats [2].
AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.
Trombodipine is an antithrombotic agent.
Vinconate is an indolonaphthyridine derivative and can stimulate the muscariic acetylcholine receptor.
K-Ras-IN-1 is a K-Ras inhibitor, by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.(the detailed information refer to the reference)
Chetoseminudin B possesses mushroom tyrosinase inhibitory activity with IC50 of 31.7 μM[1].
VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity[1][2].
L-Isovaline is a valine derivative[1].
Senecivernine is a pyrrolizidine alkaloid isolated from Senecio species, exhibits a weakly mutagenic activity[1][2].
(S)-Boc-3,4-dimethoxy-β-Phe-OH is a phenylalanine derivative[1].
Ipecoside is an alkaloid isolated from Psychotria[1].
Gefapixant citrate is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant citrate can be used for the research of chronic cough and knee osteoarthritis[1][2][3].
Zederone, a germacrane-type sesquiterpene, has potently cytotoxic against human white blood cancer cells and human prostate cancer cells. Zederone significantly inhibits the proliferation and downregulates the protein expressions of mTOR, and phosphorylated p70 S6 kinase (p-p70s6K) in SKOV3 cells[1][2].