Samelisant dihydrochloride (SUVN-G3031) is a antagonist of histamine H3 receptor with potential for the treatment of cognitive impairment, dementia, attention deficit hyperactivity disorder, epilepsy, sleep disorders, obesity, schizophrenia, eating disorders, and pain.
Human Immunoglobulin G (HumanIgG) 是一种具有保护作用的免疫球蛋白,在体液免疫中针对特定病原体(如Bacteroides forsythus和Prevotella intermedia)产生抗体反应。它可用作酶联免疫吸附试验(ELISA)的抗体标准品进行定量分析,并且Human Immunoglobulin G抗体水平在类风湿性关节炎(RA)和牙周病的研究中具有应用价值。
CAY10760 is an inhibitor of the protein-protein interaction between RAD51 recombinase and BRCA2 (EC50= 19 μM in a cell-free competitive ELISA).1It decreases homologous recombination by 54% in wild-typeBRCA2-expressing BxPC-3 pancreatic cancer cells when used at a concentration of 20 μM. CAY10760 (20 μM) decreases proliferation of BxPC-3, as well as mutantBRCA2-expressing Capan-1, cancer cells when used alone or in combination with the poly(ADP-ribose) polymerase (PARP) inhibitor olaparib . 1.Bagnolini, G., Milano, D., Manerba, M., et al.Synthetic lethality in pancreatic cancer: Discovery of a new RAD51-BRCA2 small molecule disruptor that inhibits homologous recombination and synergizes with olaparibJ. Med. Chem.63(5)2588-2619(2020)
C2 Adamantanyl globotriaosylceramide (AdaGb3) is a bioactive sphingolipid and water-soluble form of globotriaosylceramide that contains an adamantanyl group in place of the fatty acyl chain. It inhibits Vero toxin binding to globotriaosylceramide in an ELISA assay when used at a concentration of 10 μM. AdaGb3 decreases cell surface expression of P-glycoprotein (P-gp) and reduces efflux of rhodamine 123 in MDCK cells. It also increases apical-to-basal transport of vinblastine in human intestinal C2BBe1 cells.
R-8507 is a small molecule antagonist of the TNF-α type 1 receptor (TNF-αRI). It inhibits the expression of intercellular adhesion molecule-1 (ICAM-1) induced by TNF-α and IL-1β with EC50 values of 2.45 and 3.79 μM, respectively, in an ELISA using A549 lung epithelial cells.{|Gururaja2007|} It also disrupts the interaction of the TNF-αRI with receptor interacting protein 1 (RIP1) and TNF-αR-associated death domain protein (TRADD), preventing internalization of the receptor complex.
Blapsin B is a potent 14-3-3 inhibitor. Blapsin B is a naturally occurring compound isolated from the ethanol extract of the stink beetle, Blaps japanensis. Blapsin B potently inhibited 14-3-3 protein-protein interactions (PPIs) with IC(50) value of 10.0 μM as determined by an ELISA assay, and 2.5 μM in an FP assay, respectively. Blapsin B represent the first example of natural small-molecule 14-3-3 inhibitors.