Inhibitor Enzymes

Applications n-Propyl-2,2,3,3,3-d5-amine Hydrochloride is the hydrochloride salt of 1-Propyl-d5-amine (P833702); the isotope labelled analog of 1-Propylamine (P833700) which is used in the synthesis of pyrimidine derivatives as novel and highly potent PDE4 inhibitors. It is also used in the preparation of fluorenone analogs with DNA topisomerase I inhibitors.
References Goto, T. et al.: Bioorg. Med. Chem., 21, 7025 (2013); Lee, C. et al.: Bioorg. Med. Chem. 21, 7125, (2013)

Applications A labelled fatty acid found in Amaranth oil; it shows inhibitory activity.
References Fidler, N., et al.: J. Lipid Res., 41, 1376 (2000), Yang, T., et al.: Food Chem., 80, 473 (2003), Gamel, T., et al.: J. Food Lipids, 14, 323 (2007),

Applications 1-Propyl-d5-amine is labelled 1-Propylamine (P833700) which is used in the synthesis of pyrimidine derivatives as novel and highly potent PDE4 inhibitors. It is also used in the preparation of fluorenone analogs with DNA topisomerase I inhibitors.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package

Applications K252a is a protein kinase inhibitor. It is an analogue of staurosporine (S685000). It shows potent antitumor activity but no antimicrobial activity in vitro, or in vivo toxicity in rodents.
References Kase, H., et al.: J. Antibiot., 39, 1059 (1986); Yasuzawa, T., et al.; J. Antibiot., 39, 1072 (1986)

Applications N-(4'-Cyano[1,1'-biphenyl]-4-yl)-N'-[4-(3H-imidazo[4,5-b]pyridin-7-yl)phenyl] Urea, is a highly selective inhibitor of cytochrome P450 3A4, which is one of the most important enzymes involved in the metabolism of pharmaceuticals and xenobiotics.
References Song, X., et al.: Bio. Med. Chem. Lett., 22, 1611(2012);

Applications 4-Hydroxypiperidine-D4 is an isotope labelled form of 4-Hydroxypiperidine (H950845), a reagent for the synthesis of acridine (A190900) derivatives and fibrinogen receptor antagonists.
References Yang, D. et al.: Macromol., 35, 5304 (2002); Harrison, R.J. et al.: Bioorg. Med. Chem. Lett., 9, 2463 (1999);

Applications 3-Amino-N-(Tert-Butyl)Benzenesulfonamide (cas# 608523-94-0) is a useful research chemical.

Stability Moisture Sensitive
Applications rac-1,2-Dioctanoyl-3-Chloropropanediol was studied for its ability to act as an inhibitor of protein kinase C.
References Briggs, Josie C., et al.: Carbohydrate Res., 234, 23-35 (1992)

Stability Hygroscopic
Applications α-Glycosidase inhibitor.
References Jefferies, I., et al.: Bioorg. Med. Chem. Lett., 7, 1171 (1997), Hassan, A., et al.: Carbohydr. Res., 339, 1565 (2004),

Stability Hygroscopic
Applications (3R,5S,6E)-7-(2-cyclopropyl-4-phenyl-3-quinolinyl)-3,5-dihydroxy-6-heptenoic Acid Sodium Salt is an impurity of Pitavastatin (P531000), a HMG CoA reductase inhibitor and an antilipemic agent.
References Suzukim M., et al.: Bioorg. Med. Chem., 9, 2977 (1999); Yen, H., et al.: J. Clin. Invest., 98, 1253 (1996); Zou, Y., et al.: J. Biol. Chem., 274, 9760 (1999); Sun, X., et al.: Cancer Res., et al.: 61, 3382 (2001); Ladas, E.J., et al.: Clin. Oncol., 22, 517 (2004);

Applications A metabolite of the chemotherapeutic drug Tamoxifen (T006000). Exhibits a more potent estrogen agonist/antagonist activity than the parent drug. Also active as an intramembranous inhibitor of lipid peroxidation.
References Kupfer, D., et al.: Cancer Res., 54, 3140 (1994), Custodio, J.B.A., et al.: Biochem. Pharmacol., 47, 1989 (1994),

Stability Moisture Sensitive
Applications A 83-01 is a selective inhibitor of TGF-β type I receptor. A 83-01 treatment increases tumor permeability.
References Minowa, T. et al.: British. J. Canc., 101, 1884 (2009)

Applications B-[2-(Methylamino)-4-pyridinyl]boronic Acid Hydrochlroide, is used to prepare novel selective thiazoleacetic acids as CRTH2 antagonists.
References Grimstrup, M., et al.: Bioorg. Med. Chem. Lett., 20, 1181 (2010)

Applications Labelled 2-(3,4-Dimethoxyphenyl)-N-methylethylamine (D470710, free amine) which is a methylated metabolite of Dopamine (D533780); a potent inhibitor of brain mitochondrial respiration used in Parkinson’s disease studies.
References Gluck, M.R. et al.: J. Neurochem., 91, 788 (2004); Charlton, C.G. et al.: Life Sci., 66, 2159 (2000);

Applications Rhynchophylline is a novel erythropoietin-producing hepatocellular A4 (EphA4) inhibitor.
References Fu, A K.Y., et. al.: P. Natl. Acad. Sci. USA., 111, 9959 (2014)

Applications Diethyl-d10 Carbonate is deuterium labelled Diethyl Carbonate (D444000), which is used in the synthesis of 2-oxooxazolidines as antibacterials. It can also be used to synthesize donepezil/huperzine fragments as acetylcholinesterase inhibitors.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package
References Gregory, W. et al.: J. Med. Chem., 32, 1673 (1989); Bioorg. Med. Chem., 21, 676 (2013)

Stability Hygroscopic
Applications An extremely potent and selective a-D-mannosidase inhibitor.

Applications rac-syn-Ezetimibe is an analog of Ezetimibe (E975000); an antihyperlipoproteinemic and a cholesterol absorption inhibitor.
References van Heek, M., at al.: J. Pharmacol. Exp. Ther., 283, 157 (1997); van Heek, M., at al.: Brit. J. Pharmacol., 129, 1748 (2000)

Applications This compound is used in the synthesis of novel lactate dehydrogenase A inhibitors.This compound is suitable for lactate dehydrogenase (LDH) related research.
References Ward, R.A. et al.: J. Med. Chem., 55, 3258 (2012);

Applications Isotope labelled N-Fmoc-glycine is an N-Fmoc-protected form of Glycine (G615990). Glycine is a nonessential amino acid that acts as an inhibitory neyrotransmitter in the vertebrate central nervous system. Glycine also posesses cytoprotective against oxidant damage in the kidney.
References Eulenberg, V., et al.: Trend. Biochem. Sci., 30, 325 (2005); Gundersen, R., et al.: Acta Anaesth. Scand., 49, 1108 (2005); Lockart, R. & Eagle, H.: Science, 129, 252 (1959); Sogabe, K., et al.: Kidn. Int., 50, 845 (1996)

Applications GW4869 is a selective inhibitor of N-SMase.
References Lallemand, T., et al.: Arterioscler. Thromb. Vasc. Biol., 38, 1479 (2018); Figuera-Losada, M., et al.: PLoS One, 10, 0124481 (2015)