Inhibiteur d’enzymes

Stability Moisture, Temperature Sensitive; Hygroscopic
Applications A putative lipid second messenger; found to inhibit cellular mobility of melanoma cells at very low concentrations with no toxic effects thereby making it a possible agent for prevention of tumor cell metastasis and inflammatory processes. It mobilizes intracellular calcium stores, decreases cellular cAMP, activates phospholipase D and does not inhibitprotein kinase C.
References Yeh, C., et al.: Am. J. Physiol., 296, H1193 (2009), Hagen, N., et al.: J. Biol. Chem., 284, 11346 (2009), Kuehnel, M., et al.: J. Cell Sci., 122, 499 (2009),

Applications Aprotinin is used in cardiac surgery to minimize bleeding and reduce exposure to blood products.
References Mangano, D. et al.: New Eng. J. Med., 354, 353 (2006); Fergusson, D. et al.: New. Eng. J. Med., 358, 2319 (2008);

Applications An inhibitor of phosphodiesterase IV, about 8 times more active for cAMP than cGMP.
References Chesin, et al.: Biochem. Pharmacol., 21, 2443 (1972), Ahluwalia, et al.: Biochem. Pharmacol., 31, 665 (1982), Nicholson, et al.: TIPS, 12, 19 (1991),

Applications Avelstat inhibits plasma neutrophil elastase (NE) activity in zymosan-stimulated whole blood, and also inhibits NE activity on the surface of stimulated polymorphonuclear cells and in the supernatant of primed, stimulated cells.
References Stevens, T., et al.: J. Pharmacol. Exp. Ther., 339, 313 (2011)

Applications RKI-1447 is a potent and selective ROCK1 and ROCK2 inhibitor with significant anti-invasive and anti-tumor activies.
References Patel, R.A., et al.: Cancer Res., 72, 5025 (2012); Pireddu, R., et al.: Med. Chem. Comm., 3, 699 (2012)

Applications Monastrol is a small molecule that inhibits mitotic kinesin Eg5 and arrests cells in mitosis with monopolar spindles (1, 2).Monastrol is an anticancer agent against MCF-7 tumor cells (3).
References (1) Mayer, T.U., et al.: Science (1999) 286, 971 (2) Kappe, C.O., et al.: Tetrahedron (2000) 56, 1859 Marques, L.A., et al.: Naunyn-Schmiedeberg’s Arch Pharmacol (2016) [Epub ahead of print]

Applications Nicotelline is a Nicotine (N412420) related metabolite with potential as an inhibitor of human cytochrome P-450 2A6.
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 Denton, T. et al.: Biochem. Pharm., 67, 751 (2004); Gorrod, J. et al.: Anal. Det. Nic. Rel. Comp. Metab., 69, (1999);

Applications Naphthalenesulfonamides derivatives are neoplasm inhibitors.
References Hidaka, H., et al.: Proc. Nat. Acad. Sci. USA, 78, 4354 (1981)

Applications (3S,4S,3’S)-Ezetimbe is a 3-epimer impurity of Ezetimibe (E975000), 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)

Stability Hygroscopic
Applications Vitamin B12 Monocarboxylic Acid is an impurity of Vitamin B12 (V676005) which is a water-soluble vitamin with a key role in the normal functioning of the brain and nervous system, and for the formation of blood.
References Rickes, et al.: Science, 107, 396 (1948); Kirschbaum, J., et al.: Anal. Profiles Drug Subs., 10, 183 (1981); Grasbeck, R., et al.: Clin. Biochem., 17, 99 (1984)

Applications Bis(2-​butoxyethyl) 2-​(3-​Hydroxybutoxy)​ethyl Phosphate Triester is derived from 2-Butoxyethanol (B692895), which is a reagent in the synthesis of 4-butoxyethoxy-N-octadecyl-1,8-naphthalimide as a new fluorescent probe for the determination of proteins. Also used as a reagent in the synthesis of 4-hydroxybenzaldehyde derivatives as tyrosinase inhibitors.
References Sun, Y., et al.: Bioorg. Med. Chem. Lett., 21, 3798 (2011); Yi, W., et al.: Eur. J. Med. Chem., 45, 639 (2010)

Applications Benzyl Methyl Carbonate is used in designing of inhibitors for serine and thiol proteases.

Applications TBB is one of the most selective protein kinase inhibitors known, and when tested against a panel of 33 serine/threonine and tyrosine protein kinases, only three exhibited moderate inhibition by TBB, with Ki values one to two orders of magnitude higher than that for CK2.
References Boehning, D., et al.: Neuron, 40, 129 (2993)

Stability Hygroscopic
Applications A glucosidase inhibitor.
References Fellows, L.E.: Pestic. Sci., 17, 602 (1986)

Stability Hygroscopic
Applications Chelerythrine Chloride is a cell permeable protein kinase C (PKC) inhibitor.
References Song, L., et. al.: Brain Res., 1564, 52 (2014)

Applications (2R)-Pinocembrin is the (R)-enantiomer of Pinocembrin, a flavanoid with antioxidant activity found in damiana, honey, and propolis. (2R)-Pinocembrin is a potential inhibitor of PIM1 kinase, an oncogene that has been implicated in the development of leukemias, lymphomas, and prostate cancer.
References Zhao, J. et al.: J. Ethnopharmacol., 120, 387 (2008); Holder, S. et al.: Mol. Cancer Ther., 6, 163 (2007); Holder, S. et al.: Bioorg. Med. Chem., 15, 6463 (2007);

Applications Apricoxib, is an orally active, selective COX-2 inhibitor, used as as an analgesic and anti-inflammatory agent, and also has anticancer potential, since COX-2 inhibition can reduce tumor growth and augment therapy.
References Kirane, A, et al.: Clinical Cancer Res., 18, 5031 (2012); Rohatagi, Sh., et al.: British J. Clin. Pharmaco., 66, 60 (2008);

Stability Hygroscopic
Applications α-Glycosidase inhibitor.
References van de Water, F., et al.: Drug Metab. Rev., 37, 443 (2005), Koepsell, H., et al.: Pharm. Res., 24, 1227 (2007), Jappar, D., et al.: Pharm. Res., 26, 172 (2009),

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 N-Alkyl phosphoric triamide useful as urease inhibitors.

Applications tert-Butyl (2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]-2-[(1,3-thiazolidin-3-yl)carbonyl]pyrrolidine-1-carboxylate is an orally anti-diabetic agent as a inhibitors of dipeptidylpeptidase IV (DPP-4).
References Yoshida, T., et al.: Bioorg. Med. Chem., 20, 5705-5719 (2012);

Stability Light Sensitive
Applications Morusin is an inhibitor of human cervical cancer stem cell growth, attenuating NF-kB activity, and initiating apoptosis.
References Wang, L. et al.: Mol. Cell. Biochem., 379, 7 (2013);

Applications Protected Boceprevir Metabolite M4-d9 (B674522). A labelled metabolite of the Hepatitis C virus NS3 serine protease inhibitor Boceprevir (B675500). It is a COVID19-related research product.
References Venkatraman, S. et al.: J. Med. Chem., 49, 6074 (2006); Morgan, A.J, et al.: J. Lab. Cpd. Radiopharmac., 54, 613 (2011);

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)

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 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)

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)

Stability Hygroscopic
Applications Labelled (-)-Epigallocatechin Gallate, a tumor-inhibiting constituent of green tea. (-)-Epigallocatechin Gallate alters the cleavage of amyloid precursor protein, decreasing production of amaloid-ß and amaloid plaques in mice.
References Yamane, T. et al.: Cancer Res., 55, 2081 (1995); Tan, J. et al.: J. Neurosci. 25, 8807 (2005);

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

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 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 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)

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 Valtrate is a Rev-transport inhibitor with anti-HIV activity from Valerianae Radix.
References Murakami, N., et al.: Bioorg. Med. Chem. Lett., 12, 2807 (2002); Watanabe, K., et al.: Drug Discoveries Ther., 5, 26 92011)

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

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);