?PKC(85–92),Myristoylated is a cell permeable myristic acid conjugated PKC? peptide activator that enhances NO release in cultured human umbilical vein endothelial cells (HUVECs)[1].
Cimetropium Bromide is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
Oxethazaine-d6 (Oxetacaine-d6) is the deuterium labeled Oxethazaine. Oxethazaine (Oxetacaine), a precursor of phentermine acidic, is an acid-resistent and orally active analgesic agent. Oxethazaine (Oxetacaine) has the potential for the relief of pain associated with peptic ulcer disease or esophagitis[1][2].
MMP-9/MMP-13 Inhibitor I is a potent MMP-9 and MMP-13 inhibitor with IC50s of both 0.9 nM. MMP-9/MMP-13 Inhibitor I shows >20-folds selectivity for MMP-9/MMP-13 over other MMPs[1].
Asthma relating compound 1 is an anti-asthmatic agent candidate extracted from patent EP0295656A1.
Apigenin-4'-α-L-rhamnoside is a potent inhibitor of HBV. Apigenin-4'-α-L-rhamnoside inhibits the secretory level of HBV surface antigen (HBsAg) in HepG2.2.15 cells[1].
Captopril disulfide is a metabolite of Captopril with antihypertensive activity[1].
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying[1][2][3].
TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death[1].
Corysamine is an alkaloid derived from Stylophorum lasiocarpum[1].
UNC 0631 is a potent G9a inhibitor with IC50 value of 4 nM.IC50 value: 4 nM [1]Target: G9aUNC 0631, which had high in vitro potency versus G9a and improved lipophilicity, was highly potent (IC50 < 0.06 μM) in reducing H3K9me2 levels in MDA-MB-231 cells and had low cell toxicity. In particular, compounds 7 was more potent than compound 5 and had a similar tox/function ratio in MDAMB-231 cells. UNC 0631 showed excellent separation of functional potency versus cell toxicity in MDA-MB-231 cells, thecompound was further evaluated in a variety of cell lines to characterize it's cellular potency and cell toxicity. UNC 0631 had excellent tox/functionratios in these cell lines.
LY2940094 is a potent, selective and orally available nociceptin receptor (NOP) antagonist with an Ki of 0.105 nM.
Xanthoxylin (Xanthoxyline) is isolated from Zanthoxylum simulans. Xanthoxylin (Xanthoxyline) has antifungal and antispasmodic activities[1][2].
Mag-fura-2 AM is a membrane osmotic fluorescent indicator of intracellular magnesium. Mag-fura-2 AM can enter cells by incubation and is hydrolyzed to Mag-fura-2 by cellular esterases. (λex=340 nm, λem=510 nm)[1].
Ru-32514 is an agonist of benzodiazepine receptor.
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities[1].
Flibanserin (BIMT-17; BIMT-17BS) hydrochloride is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin hydrochloride binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin hydrochloride shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research[1]-[5].
CDK2 is a member of the eukaryotic S/T protein kinase family and its function is to catalyze the phosphoryl transfer of ATP γ-phosphate to serine or threonine hydroxyl (denoted as S0/T0) in a protein substrate.
H-allo-Thr(tBu)-OH is a threonine derivative[1].
Suc-Val-Pro-Phe-pNA is a substrate for cathepsin G and can be used to detect the activity of this enzyme[1].
HMBR, an analog bearing an additional methyl group on the aromatic ring, is nonfluorescent by itself, but it fluoresces yellow light upon blue-light excitation when bound to Y-FAST. HMBR is nontoxic for zebrafish embryos. cell-permeant[1].
(2’,3’,5’-Tri-O-acetyl)uridine 5-carboxylic acid 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].
GDC-0310 is a selective acyl-sulfonamide Nav1.7 inhibitor, with an IC50 of 0.6 nM for hNav1.7[1].
Taurochenodeoxycholic acid is one of the main bioactive substances of animals' bile acid.
Pomalidomide-PEG2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology[1].
Z-Ser-OMe is a serine derivative[1].
NH-bis(PEG3-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Hydroxy-PEG1-C2-methyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Ethylhexadecyldimethylammonium (EHDA) bromide, a surfactant, has been used in a number of adsorptive separational methods, such as the removal of nickel, zinc and chromium ions. Ethylhexadecyldimethylammonium (EHDA) bromide also can be used to prepare dye of staining intracellular ions[1][2].
Pseudolaric Acid B is a diterpene isolated from the root of Pseudolarix kaempferi Gorden (pinaceae), has anti-cancer, antifungal, and antifertile activities, and shows immunosuppressive activity on T lymphocytes[1][2][3]. Pseudolaric Acid B inhibits hepatitis B virus (HBV) secretion through apoptosis and cell cycle arrest. Pseudolaric Acid B induces autophagy[4][5].