Tulmimetostat is an antineoplastic[1].
PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 uM, respectively.IC50 value: 5.6/7.9 uM ( recombinant mouse/ human GPR119) [1]Target: GPR119 agonistSystemic administration of PSN632408 (30 mg/kgintraperitoneally) suppresses food intake, reduces weight gain, and white adipose tissue deposition in rats. GPR119 (previously designated SNORF25) is an orphan G protein-coupled receptor expressed predominantly in the pancreas and gastrointestinal tract in humans and in the brain, pancreas, and gastrointestinal tract in rodents. It mediates a reduction in food intake and body weight gain in rats upon treatment with oleoyl ethanolamide (OEA), an endogenous, potent agonist for PPARα. These data suggest that PSN632408 may be useful as a therapeutic agent for the treatment of obesity.
MS-PEG10-THP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Sampeginterferon beta-1a (BCD-054) is a pegylated IFNβ-1a. Sampeginterferon beta-1a can be used for research against remitting multiple sclerosis[1][2].
2-Hydroxyalbrassitriol (Compound 6) is an AChE inhibitor with an IC50 of 35.97 μM[1].
8-Methylsulfinyloctyl isothiocyanate, an isothiocyanate, has antimicrobial activity and remarkable inhibitory activity against plant growth[1]. 8-Methylsulfinyloctyl isothiocyanate impair COX-2 mediated inflammatory responses in LPS stimulated raw macrophages[2].
N-(Azido-PEG3)-N-bis(PEG3-acid) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Valorphin is an endogenous hemoglobin β-chain (33-39) fragment with opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM; Valorphin also shows anti-tumor activity.
Platyphyllonol (Platyphyllone) can be isolated from A. japonica. Platyphyllonol shows cytotoxic effects on MCF-7 cells with IC50 values of 46.9 μg/mL[1].
TAK-676 is an agonist of STING, triggering the activation of STING signaling pathway and type I interferons. TAK-676 is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. TAK-676 promotes durable IFN-dependent antitumor immunity[1].
Flizasertib is a serine/threonine kinase inhibitor[1].
Ammonium chloride, as a heteropolar compound with pH value regulation, can cause intracellular alkalization and metabolic acidosis thus effecting enzymatic activity and influencing the process of biological system. Ammonium chloride is an autophagy inhibitor[1][2].
Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor. Microtubule inhibitor 4 shows cytotoxicity with IC50s of 4.0, 3.2, 2.1 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 4 shows the inhibition of tubulin polymerization[1].
S1P1 agonist 4 has a better profile in both potency (EC50 < 0.05 mg/kg) and predicted human half-life (t1/2 ∼ 5 days).
Pendulone is a isoflavanquinone with good antiplasmodial activity with an IC50 of 7.0 µM. Pendulone also has antileishmanial, antibacterial and anticancer activity[1][2].
Dehydroaripiprazole-d8-1 is the deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1] [2] [3] [4] .
Potassium thiocyanate-13C is the 13C labeled Potassium thiocyanate[1].
Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin can be used to synthesize chemical probes toward PEBP-proteins. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice [1][2][3].
WAY-648936 is an active molecule.
Adenosine is a nucleoside composed of a molecule of adenine attached to a ribose sugar molecule (ribofuranose) moiety via a β-N9-glycosidic bond.Target: Nucleoside antimetabolite/analogAdenosine plays an important role in biochemical processes, such as energy transfer — as adenosine triphosphate (ATP) and adenosine diphosphate (ADP) — as well as in signal transduction as cyclic adenosine monophosphate, cAMP. It is also an inhibitory neurotransmitter, believed to play a role in promoting sleep and suppressing arousal. Adenosine also plays a role in regulation of blood flow to various organs through vasodilation.Adenosine is an endogenous purine nucleoside that modulates many physiological processes. Cellular signaling by adenosine occurs through four known adenosine receptor subtypes. Extracellular adenosine concentrations from normal cells are approximately 300 nM; however, in response to cellular damage (e.g. in inflammatory or ischemic tissue), these concentrations are quickly elevated (600–1,200 nM). Thus, in regard to stress or injury, the function of adenosine is primarily that of cytoprotection preventing tissue damage during instances of hypoxia, ischemia, and seizure activity. Activation of A2A receptors produces a constellation of responses that in general can be classified as anti-inflammatory.
Peptide YY (13-36) (canine, mouse, porcine, rat) is a Y2 receptor subtype agonist[1].
(R)-Pirtobrutinib ((R)-LOXO-305) is a less active enantiomer of Pirtobrutinib. Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations[1].
Meglutol-d3 is the deuterium labeled Meglutol[1]. Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutarryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol.
Isograndifoliol is a selective inhibitor of butyrylcholinesterase (BChE) with an IC50 value of 0.9 μM. And Isograndifoliol moderately inhibits acetylcholinesterase (AChE) with an IC50 value of 342.9 μM. Isograndifoliol also has vasorelaxant effect and anti-tumor effect. Isograndifoliol can be used for research against dementia caused by neurodegenerative diseases[1][2][3].
Inflachromene (ICM) is a microglial inhibitor with anti-inflammatory effects, directly binds high mobility group protein 1 (HMGB1) and HMGB2 and reduces their cytoplasmic accumulation in microglial cells; blocks the sequential processes of cytoplasmic localization and extracellular release of HMGBs by perturbing its post-translational modification; effectively downregulates proinflammatory functions of HMGB and reduces neuronal damage in vivo.
Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC50 of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
1-Pyrenebutyric acid is a fluorescence probe that can be used in fluorescence determination of DNA. 1-Pyrenebutyric acid can be used as a linker for biomolecules to form a self-assembled monolayer on grapheme[1].
5-Hydroxyomeprazole-d3-1 is the deuterium labeled 5-Hydroxyomeprazole[1].
Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.
ROS kinases-IN-2 is a ROS kinase inhibitor with 21.53% inhibition at 10 μM[1].