Inhibitor Enzymes

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 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)

Applications CP-10447 is an inhibitor apolipoprotein B (apoB) and triglyceride secretion in human hepatoma cells (HepG2) by inhibiting MTP activity and stimulating the early ER degradation of apoB. It is useful tool for further study of the mechanisms of apoB secretion and triglyceride-rich lipoprotein assembly.
References Haghpassand, M. et al.: J. Lipid. Res., 37, 1468 (1996); Pan, M. et al.: J. Biol. chem., 275, 27399 (2000);

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)

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 O-(2,4-Dinitrophenyl)hydroxylamine is a rapid active-site-directed inhibitor of D-amino acid oxidase; modification results in specific incorporation of an amine group into an accessible nucleophilic residue with concomitant release of 2,4-dinitrophenol.
References D'Silva, C., et al.: Biochemi., 25, 5602 (1986),

Applications (3R)-1-Methyl-3-Pyrrolidinemethanol is a reactant in the synthesis of heterocyclic carboxylic acid amides with potential as PDK1 inhibitors.

Stability Hygroscopic
Applications N-Acetyl-Phe-Octreotide is used as reactant/reagent in inhibition of octreotide acylation inside PLGA microspheres by derivatization of amines of peptide with self-immolative protecting group.
References Shirangi, M., et al.: Bioconjugate Chem., 27, 576-585 (2016)

Applications Curcumin (C838500) and gingerdione derivative. A possible human glyoxalase I inhibitor. Flavor modifier.
References Yuan, M. et al.; Bioorg. Med. Chem. 19, 1189 (2011); Ley, J. et al.; J. Agr. Food Chem. 56, 6656 (2008)

Stability Moisture and Temperature Sensitive
Applications Galacto-PUGNAc is a highly selective inhibitor for β-hexosaminidases HEXA and HEXB is cell-permeable. Galacto-PUGNAc is able to modulate the activity of HEXA and HEXB in tissue culture, increasing ganglioside GM2 levels in neuroblastoma cells
References Stubbs, K.A. et al.: Angew. Chem. Int. Ed., 48, 1300 (2009);

Applications (±)-Procinolol is a beta adrenergic receptor antagonist.
References Singh, K.: Indian J. Phsiol. Pharmacol., 27, 311 (1983)

Applications An analogue of Olomoucine (Cat. # O567000) that acts as a potent inhibitor of Cdk 1 (IC50=100nm) and Cdk2 (IC50=80nm). Also displays antiproliferative and proapoptotic effects.
References Wermeulen, K., et al.: Leukemia, 16, 299(2002)

Applications HS-173 is a potent PI3Kα inhibitor with anticancer activity.
References Kim, O., et al.: J. Med. Chem., 54, 2455 (2011); Lee, H., et al.: Cancer Lett., 328, 152 (2013)

Applications AZD3839 is a potent and selective inhibitor of human Beta-secretase 1 (BACE1).
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 Jeppsson, F., et al.: J. Biol. Chem., 287, 41245 (2012)

Applications Baohuoside I is an inhibitor of cell growth and also is a down-regulator of durvivin and cyclin D1 expression. Used in the treatment of esophageal cancer. Anti-cancer agent.
References Lifang, W. et al.: Oncology Rep., 26, 1149 (2011); Jin, X. et al.: Drug Dev. Ind. Pharm., 39, 1421 (2013);

Applications A pyrimidine derivative as G protein-coupled receptor kinase (GRK) inhibitor.
References Bigham, E., et al.: J. Med. Chem., 35, 1399 (1992), Jansen, M., et al.: Biochem. Pharmacol., 47, 1067 (1994), Hasbi, A., et al.: J. Neurochem., 70, 2129 (1998),

Applications Wiskostatin is an selective inhibitor of neural Wiskott-Aldrich syndrome protein (WASP).
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 Peterson, J.R., et al.: Nat. Struct. Mol. Biol., 11, 747 (2004)

Applications Found to have a potent inhibitory action against casein kinase 1 completely with respect to ATP and a much weaker effect on casein kinase 2 and other protein kinases.
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 Hidaka, H., et al.: J. of Biol. Chem., 264, 9, 4924 (1989)

Applications A highly potent (IC50=1.5nM) and uniquely specific tyrosine kinase inhibitor of a rationally engineered v-Src tyrosine kinase.
References Bishop, A.C., et al.: J. Am. Chem. Soc., 121, 627 (1999)

Applications Retorphan is a powerful and selective inhibitors of neprilysin and is being developed as a therapeutic agent. Retorphan behave as the prodrug of the enantiomers of Thiorphan (T369500).
References Monteil, T., et al.: Mini. Rev. Med. Chem., 2, 209 (2002); Roques, B.P., et al.: Nature, 288, 286 (1980); Tiraboschi, G., et al.: Protein Engineering, 12, 2, 141 (1999)

Applications A cyclopentanamine used in the preparation of heterocyclic and aromatic ureas and amides as CEPT inhibitors.

Applications LB 42708 is a selective nonpeptidic Farnesyltransferase (FTase) inhibitor.LB42708 suppresses tumor growth and tumor angiogenesis in both xenograft tumor models of Ras-mutated HCT116 cells and its wild-type Caco-2 cells, indicating its potential application in the treatment of both Ras-mutated and wild type tumors.
References Kim, C., et. al.: Mol. Pharmacol., 78, 142 (2010)

Applications Propargyl Alcohol-13C3 is labelled Propargyl Alcohol (P762550) which is used as a corrosion inhibitor, a metal complex solution, a solvent stabilizer and an electroplating brightener additive. It is also used as an intermediate in organic synthesis.
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 Zhang, T., et al.: Res. Chem. Interm. (2013); Choudhary, Y., et al.: SPE Product. Operat., 28, 268 (2013); Hed, Y., et al.: J. Mater. Chem. Mater. Bio. Med., 1, 6015 (2013)

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 Raloxifene 4’-Glucuronide Lithium Salt is a metabolite of Raloxifene (R099995), a nonsteroidal estrogen receptor mixed agonist/antagonist.
References Dodge, J., et al.: Bioorg. Med. Chem. Lett., 7, 993 (1997); Jeong, E., et al.: Drug Metab. Dispos., 33, 785 (2005); Trontelj, J., et al.: Pharmacol. Res., 52, 334 (2005); Oswald, S., et al.: Clin. Pharmacol. Ther., 79 206 (2006)

Applications HX 531 is a novel RXR antagonist used to enhance transactivation of PPARγ and ST 13 preadipocyte differentiation. Helps in the reduction of triglyceride content in white adipose tissue, skeletal muscle and liver.
References Yamauchi, T. et al.: J. Clin. Invest., 108, 1001 (2001);

Applications N-[4-Amino-2-chloro-6-[(2-deoxy-2-fluoro-β-D-arabinopyranosyl)amino]-5-pyrimidinyl]-formamide is a clofarabine related compound. Clofarabine (C586890) is a second generation purine nucleoside analog; antimetabolite that inhibits DNA synthesis and resists deamination by adenosine deaminase. Antineoplastic.
References Gandhi, V., et al.: Clin. Cancer Res., 9, 6335 (2003), Kantarjian, H., et al.: Blood, 102, 2379 (2003), Faderl, S., et al.: Cancer, 103, 1985 (2005),

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),

Applications 4-Fluorobenzoic Acid-d4 is used as a reagent in the synthesis of Flurofamide-d4 (F596687); the isotope labelled analog of Fluorofamide (F596685) which is a compound that acts as a urease inhibitor, useful in the treatment of gastritis and irregular urease activity in the urinary tract.
References Loes, A. et al.: Lett. App. Microbiol., 58, 31 (2014); Ohta, T.et al.: Biochem. Biophys, Res. Comm., 285, 728 (2001)

Applications n-Pentyl-d11 chloroformate is labelled n-Pentyl chloroformate which can be used to synthesize 1,3-disubstituted ureas as potent inhibitors of the soluble epoxide hydrolase.
References Kim, I., et al.: J. Med. Chem., 47, 2110 (2004); Hammock, B., et al.: PCT Int. Appl. (2006), WO 2006045119 A2 20060427.

Stability Air and Moisture Sensitive
Applications N-[4-Amino-2-chloro-6-[(2-deoxy-2-fluoro-α-D-arabinopyranosyl)amino]-5-pyrimidinyl]-formamide is a clofarabine related compound. Clofarabine (C586890) is a second generation purine nucleoside analog; antimetabolite that inhibits DNA synthesis and resists deamination by adenosine deaminase. Antineoplastic.
References Gandhi, V., et al.: Clin. Cancer Res., 9, 6335 (2003), Kantarjian, H., et al.: Blood, 102, 2379 (2003), Faderl, S., et al.: Cancer, 103, 1985 (2005),

Applications 4-​Pyridin-​2,​3,​5,​6-​d4-​ol-​d is one of the azepanone derivatives studies as CGRP receptor antagonists.
References Liu, J.: PCT Int. Appl. (2010), WO 2010108103 A1 20100923.

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 Isotope labelled O-Desethyl Azilsartan is an active metabolite of TAK-491 which acts as a new angiotensin II receptor antagonist.
References Kawaguchi, N. et al.: Xenobiotica, 43, 182 (2013);

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),

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 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 Ceramide-1-phosphate blocks apoptosis through inhibition of acid sphingomyelinase in macrophages.
References Furukawa, A., et al.: Mol. Cell. Biochem., 305, 27 (2007), Chen-Quay, S., et al.: J. Pharm. Sci., 98, 606 (2009),

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);

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);