Trt-PEG4-C2-acid (hydrate) is a polyethylene glycol (PEG)-derived linking moiety, specifically designed for the synthesis of Proteolysis Targeting Chimeras (PROTACs).
α-Cyclodextrin (α-CD) is a saccharide comprised of six glucose subunits linked by α-1,4 bonds, which results in a cone-shaped molecule.1It contains a hydrophobic interior and hydrophilic exterior, which allow it to form inclusion complexes with wide variety of molecules, conferring enhanced solubility and stabilization to the molecules. α-CD has commonly been used in the separation and purification of chemicals on an industrial scale.1,2Formulations containing α-CD have been used in the pharmaceutical industry to improve the physical and chemical properties of compounds, the food industry as flavor carriers and stabilizers in processed and ultra-processed foods and certain beverages, as well as in other industrial applications. 1.Li, S., and Purdy, W.C.Cyclodextrins and their applications in analytical chemistryChem. Rev.92(6)1457-1470(1992) 2.Astray, G., Gonazalez-Barreiro, C., Mejuto, J.C., et al.A review on the use of cyclodextrins in foodsFood Hydrocolloids23(7)1631-1640(2009)
DX-9065A is a factor Xa inhibitor. DX-9065a inhibits proinflammatory events induced by factor Xa and gingipains. DX-9065a is a competitive inhibitor of the Spectrozyme FXa (SpFXa) cleavage by both fXa and prothrombinase with similar K(i) values of approxi
UDP-Glucuronic acid is a nucleoside diphosphate sugar that is a source of glucuronic acid for polysaccharide biosynthesis. This compound can be used for the formation of many glucuronides with various aglycones.1 1.Green, M.D., and Tephly, T.R.Glucuronidation of amine substrates by purified and expressed UDP-glucuronosyltransferase proteinsDrug Metab. Dispos.26(9)860-867(1998)
Tigecycline hydrate (GAR-936 hydrate) is a broad spectrum glycylcycline antibiotic. Tigecycline hydrate is bacteriostatic, that inhibits protein synthesis by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline hydrate is active against resistant strains of Gram-positive and Gram-negative bacteria .
Adenosine 5’-methylenediphosphate is an inhibitor of ecto-5’-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5’-monophosphate , adenosine 5’-diphosphate , or adenosine 5’-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5’-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) cells in a migration assay.2,3It increases tumor infiltration of CD3+CD8+T cells and reduces tumor growth in a K1735 murine melanoma model when administered at a dose of 400 μg mouse.4 1.Bruns, R.F.Adenosine receptor activation by adenine nucleotides requires conversion of the nucleotides to adenosineNaunyn Schmiedebergs Arch. Pharmacol.315(1)5-13(1980) 2.Braganhol, E., Tamajusuku, A.S.K., Bernardi, A., et al.Ecto-5′-nucleotidase CD73 inhibition by quercetin in the human U138MG glioma cell lineBiochim. Biophys. Acta1770(9)1352-1359(2007) 3.Shali, S., Yu, J., Zhang, X., et al.Ecto 5′ nucleotidase (CD73) is a potential target of hepatocellular carcinomaJ. Cell Physiol.234(7)10248-10259(2018) 4.Forte, G., Sorrentino, R., Montinaro, A., et al.Inhibition of CD73 improves B cell-mediated anti-tumor immunity in a mouse model of melanomaJ. Immunol.189(5)2226-2233(2021)
Meclofenamate sodium is a potent non-steroidal anti-inflammatory agent, which can specifically inhibit chemokine-induced human polymorphonuclear leukocyte function: chemotaxis, degranulation, and superoxide anion free radical production.
Pancuronium is an aminosteroid antagonist of muscle-type nicotinic acetylcholine receptors (nAChRs) with an IC50value of 14.8 nM using patch clamp electrophysiology in BOSC23 cells expressing mouse nAChRs.1It acts as a non-depolarizing neuromuscular blocking agent.2Pancuronium enhances anesthesia induced by isoflurane , reducing immobilization with an ED50value of 1.62 μg kg.3 1.Liu, M., and Dilger, J.P.Site selectivity of competitive antagonists for the mouse adult muscle nicotinic acetylcholine receptorMol. Pharmacol.75(1)166-173(2009) 2.Buckett, W.R., Marjoribanks, C.E., Marwick, F.A., et al.The pharmacology of pancuronium bromide (Org.NA97), a new potent steroidal neuromuscular blocking agentBr. J. Pharmacol. Chemother.32(3)671-682(1968) 3.Miyazaki, Y., Sunaga, H., Hobo, S., et al.Pancuronium enhances isoflurane anesthesia in rats via inhibition of cerebral nicotinic acetylcholine receptorsJ. Anesth.30(4)671-676(2016)
3-O-methyl-L-DOPA is a metabolite of L-DOPA , produced by the activity of catechol O-methyltransferase. 3-O-methyl-L-DOPA may have effects of its own or it may compete with the actions of L-DOPA.
HPI-1 (hydrate) is a Hedgehog (Hh) pathway inhibitor that suppresses signaling through Sonic Hh (IC50= 1.5 μM) without significantly affecting Wnt signaling (IC50≥ 30 μM).1HPI-1 suppresses Hh activation induced by loss of Suppressor of Fused or by Gli overexpression, suggesting action at posttranslational modification of Gli protein or at the interaction of Gli with a co-factor.1HPI-1 (hydrate) also inhibits signaling through the oncogenic Smoothened (Smo) mutant SmoM2 in neuron precursors, preventing cell proliferation.1 1.Hyman, J.M., Firestone, A.J., Heine, V.M., et al.Small-molecule inhibitors reveal multiple strategies for Hedgehog pathway blockadeProceedings of the National Academy of Sciences of the United States of America106(33)14132-14137(2009)
Cefsulodin is a β-lactam antibiotic that lyses actively-growingE. coliby binding specifically to the intermembrane proteins, penicillin-binding proteins 1a and b, whose transglycosylase and transpeptidase activities are involved in cell elongation and septation.1Cefsulodin has been used in combination with other β-lactam antibiotics, such as cefazolin as a strategy to circumvent drug resistance.2
Quinacrine is a compound that is commonly used as an anti-protozoal agent. It inhibits voltage-dependent sodium channels (IC50: 3.3 μM) and suppresses aldehyde oxidase (IC50: 3.3 μM). Quinacrine prevents misfolding of prion protein (EC50: 0.3 μM). As an e