β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold)[1].
Aristolactam BIII is a potent DYRK1A inhibitor and inhibits the kinase activity of DYRK1A in vitro (IC50= 9.67 nM. Aristolactam BIII rescues the proliferative defects of DYRK1A transgenic (TG) mouse-derived fibroblasts and neurological and phenotypic defects of DS-like Drosophila models[1].
Indirubin(Couroupitine B) is a purple 3,2- bisindole and a stable isomer of indigo isolated from Indigo naturalis (Apiaceae); anti-inflammatory and anticancer activities.IC50 value:Target:in vitro: The activation of EGF receptor, known to be highly expressed in psoriatic lesions, was inhibited by indigo naturalis or indirubin. The cell proliferation and CDC25B expression of epidermal keratinocytes were induced by EGF alone and confirmed to be inhibited by indigo naturalis or indirubin [2]. indirubin inhibited prostate tumor growth through inhibiting tumor angiogenesis. indirubin inhibited angiogenesis in vivo. We also showed the inhibition activity of indirubin in endothelial cell migration, tube formation and cell survival in vitro [3].in vivo: Indirubin treatment suppressed skin inflammation in DNCB-exposed mice. The skin lesions were significantly thinner in the Indirubin-treated group than in untreated controls, and the hyperkeratosis disappeared. Indirubin reduced the total serum IgE level and cytokines production. In addition, it normalized NF-κB, IκB-α and MAP kinase expression [1]. Indirubin dose-dependently inhibited intersegmental vessel formation in zebrafish embryos. It also inhibited HUVEC proliferation by the induction of cellular apoptosis and cell-cycle arrest at the G0/G1 phase [4].
AR7 is a retinoic acid receptor α (RARα) antagonist.
(S)-Falcarinol (Panaxynol), one of the major polyacetylenes isolated from Panax ginseng, has antitumor activity. (S)-Falcarinol (Panaxynol) is the most potent antiplatelet agent in ginseng and its mechanism of action is chiefly due to the inhibition of thromboxane formation. (S)-Falcarinol (Panaxynol) is a potent Nrf2 activator[1][2][3].
1-hexadecyl-2-azelaoyl-sn-glycero-3-phosphocholine is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Peptide R, a cyclic peptide, is a specific CXCR4 antagonist. Peptide R shows outstanding capacities to profoundly remodel the tumor stroma. Peptide R has the potential for tumor research[1][2].
Aspartyl-alanyl-diketopiperazine (DA-DKP) is an immunomodulatory molecule generated by cleavage and cyclization from the N-terminus of human albumin and can modulate the inflammatory immune response through a molecular pathway implicated in T- lymphocyte anergy[1][2].
Efalizumab is a targeted T cell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits T cell activation, cutaneous T cell trafficking, and T cell adhesion to keratinocytes, can be used for plaque psoriasis research[1].
GEMSA is a potent inhibitor of enkephalin convertase (Ki=8.8 nM). GEMSA elicites analgesia[1].
Efaproxiral is a synthetic allosteric modifier of haemoglobin (Hb), decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy.in vitro: Efaproxiral increases oxygen levels in hypoxic tumor tissues by binding non-covalently to the hemoglobin tetramer and decreasing hemoglobin-oxygen binding affinity. Increasing tumor oxygenation reduces tumor radioresistance. Efaproxiral can enhance the oxygenation of hypoxic tumours and function as a radiation sensitiser, increasing the effectiveness of RT.
Ganglioside GM3 is a precursor of a-, b-, and c-series gangliosides, interacts with transmembrane receptors such as the epidermal growth factor and insulin receptors, and regulates receptor functions by creating a specialized lipid environment. Ganglioside GM3 is synthesized by GM3 synthase and can be used for the research of hypercholesterolemia[1].
Voacamine, an indole alkaloid, isolated from Voacanga Africana, exhibits potent cannabinoid CB1 receptor antagonistic activity[1]. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells[1].
APTO-253 is an inducer of Kruppel-like factor 4 (KLF4), and also stabilizes Gquadruplex, with anti-proliferative activity.
Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD+-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM[1].
Salviolone is a natural diterpenoid derivative that can against melanoma cells. Salviolone exhibits a pleiotropic effect against melanoma by hampering cell cycle progression, STAT3 signaling, and malignant phenotype of A375 melanoma cells[1].
PDD00031705 is a benzimidazolone core cell-inactive inhibitor of Poly (ADP-ribose) glycohydrolase (PARG)[1].
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects[1].
Cy5 DBCO chloride is an azide reaction probe and the addition of DBCO molecules allows the imaging of azide-labelled biomolecules by a copper-free “Click Chemistry” reaction[1].
alpha-1,2-Fucosyltransferase (α1,2FucT), i.e., alpha 1, 2-fucosyltransferase, is often used in biochemical studies. alpha-1,2-Fucosyltransferase is a rate-limiting enzyme, can catalyze the synthesis of Lewis y (a cell membrane-associated carbohydrate antigen)[1].
5-Amino-8-hydroxyquinoline (5A8HQ), a potential anticancer candidate, has promising proteasome inhibitory activity.
T808 is a tau-selective Alzheimer’s PET ligand. T808 is a type of imaging agent used in positron emission tomography (PET) scans. It is a radiotracer that is used to help visualize certain areas of the body, such as the brain, in order to diagnose and monitor various medical conditions[1].
PI3Kδ-IN-9 is a selective PI3Kδ inhibitor with an IC50 value of 3.8 nM.
Me-CO-Lys(Cbo)-Gly-Arg-pNA is a substrate for C1 esterase[1].
ATR-IN-6 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-6 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent WO2021233376A1, compound A22)[1].
Fura Red is a Ca2+-sensitive fluorescent dye, which decreases in fluorescence with rising [Ca2+][1].
hDDAH-1-IN-1 TFA (compound 8a) is a potent and selective non-amino acid catalytic site inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1), with a Ki of 18 µM[1].
Xenalamine is a synthetic antiviral agent.
Lauric acid-13C-1 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively[1].
Obiltoxaximab is a potent anti-protective antigen (PA) monoclonal antibody. Obiltoxaximab plays a central role in anthrax toxin assembly and target cell intoxication. Obiltoxaximab can be used in animal‐to‐human dose translation for treatment of inhalational anthrax[1][2].