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.
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].
Xenalamine is a synthetic antiviral agent.
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].
Fura Red is a Ca2+-sensitive fluorescent dye, which decreases in fluorescence with rising [Ca2+][1].
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].
(Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity[1][2].
2-Hydroxycinnamaldehyde is a phenylpropanoid that can be isolated from the bark of Cinnamomum cassia. 2-Hydroxycinnamaldehyde inhibits Wnt/β-catenin, STAT3 signaling. 2-Hydroxycinnamaldehyde induces cell apoptosis 2-Hydroxycinnamaldehyde has antitumor and anti-inflammation activities[1][2][3].
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].
(R)-6',7'-Dihydroxybergamottin ((R)-6′,7′-DHB) is a competitive inhibitor of human and rat CYP1A1 activity with Kis of 55 μM and 1.72 μM, respectively. (R)-6',7'-Dihydroxybergamottin has the potential for cancer research[1].
Lysostaphin is an antistaphylococcal agent. Lysostaphin has activities of three enzymes namely, glycylglycine endopeptidase, endo-β-N-acetyl glucosamidase and N-acteyl muramyl-L-alanine amidase[1].
Cysteamine S-phosphate (Cystaphos) sodium can be hydroIyzed to Cysteamine by human alkaline phosphatases. Cysteamine is an orally active agent for the research of nephropathic cystinosis and an antioxidant[1][2].
5(6)-Carboxyfluorescein contains a carboxylic acid that can be used to react with primary amines via carbodiimide activation of the carboxylic acid; cell-impermeant 5,6-FAM can also be used as a nonfixable polar tracer to investigate fusion, lysis and gap-junctional communication and to detect changes in cell or liposome volume.
Fmoc-EDA-N3 is a click chemistry reagent containing an azide group[1].
Etbicyphat (Trimethylopropane phosphate) is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1].
Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist[1].
MLN 3897 is a potent, specific and orally active antagonist of CCR1 with IC50 of 0.8 nM in competition binding assays, 500-fold selectivity over CCR5; inhibits osteoclastogenesis and OC activity by impairing multinucleation and by down-regulation of c-fos signaling, inhibits osteoclastogenesis and OC activity by impairing multinucleation and by down-regulation of c-Fos signaling; demonstrates potential for the treatment of multiple sclerosis and rheumatoid arthritis. Multiple Sclerosis Phase 1 Discontinued
3',4',7-Trimethoxyquercetin (Quercetin 3′,4′,7-trimethyl ether) is a polymethoxylated flavone isolated from the plant of genus Taraxacum, has antioxidant activity[1].
Sotuletinib (BLZ945) dihydrochloride is an orally active and blood-brain barrier-permeable CSF1-R-specific inhibitor (IC50=1 nM). Sotuletinib (BLZ945) dihydrochloride induces tumor cell apoptosis and effectively inhibits tumor growth in mouse models. Sotuletinib dihydrochloride can be used in cancer and amyotrophic lateral sclerosis (ALS) research[1].
1-(3-Beta-amino-2,3-dideoxy-beta-d-threopenta-furanosyl)thymine 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].