Inhibitor Enzymes

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);

Stability Hygroscopic
Applications An inhibitor of fatty acid oxidation. Aminocarnitine acts as a hypoglycemic and antiketogenic compound. It alters lipidic metabolism by inhibiting carnitine acetyltransferase (CAT) and carnitine palmitoyltransferase (CPT).
References Jenkins, D.L., et al.: J. Biol. Chem., 260, 14748 (1985), Kanamaru, T., et al.: M. Life Sci., 37, 217 (1985), Hulsmann, W.C., et al.: J. Biochim. Biophys. Acta., 1097, 263 (1991), Chiodi, P., et al.: Biochim, Biophys. Acta., 1127, 81 (1992),

Applications Teneligliptin Hydrobromide (2:5) is a dipeptidyl peptidase-4 (DPP-4) inhibitor that is used to treat type 2 diabetes. It is eliminated via excretion, and has a half-life of 24.2 hours in the human body.
References Goda, M. & Kadowaki, T.: Drugs Today, 49, 615 (2013); Kishimoto, M.: Diabetes Metab. Syndr. Obes., 6, 187 (2012)

Stability Light Sensitive
Applications β-Cembrenediol is an inhibitor of tumor promotion. Novel c-Met inhibitors which are used in anticancer treatments.
References Le-Huu, P. et al.: ChemCatChem., 8, 3755 (2016); Ebrahim, H. et al.: Bioorg. Med. Chem., 24, 5748 (2016);

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 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),

Applications 2-(Hydroxyamino)acetic Acid is a novel lactase inhibitor.
References Hattori, M., et al.: J. Insect Physiol., 51, 1359 (2005); Murao, S., et al.: Biosci. Biotech. Biochem., 56, 987 (1992)

Applications N-Alkyl phosphoric triamide useful as urease inhibitors.

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)

Applications Nitromifene citrate is a non-steroidal estrogen antagonist. It is structurally similar to Tamoxifen (T006000) which is a selective estrogen response modifier (SERM).
References Rudick, C., et al.: Endorcrinol., 144, 179 (2003); Sutherland, R., et al.: Nature, 267, 434 (1977)

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

Impurity Atorvastatin Related Compound E
Applications Impuritiy of Atorvaststin (A791750), a selective, competitive HMG-CoA reductase inhibitor. Atorvastatin is the only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia. Atorvastatin Related Compound E
References Kearney, A.S., et al.: Pharm. Res., 10, 1461 (1993), Heinonen, T.M., et al.: Clin. Ther., 18, 853 (1996), Whitfield, L.R., et al.: Eur. J. Drug Metab. Pharmacokinet., 25, 97 (2000),

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 Labelled Curcumin (C838500). A natural phenolic compound. Potent anti-tumor agent having anti-inflammatory and anti-oxidant properties. Induces apoptosis in cancer cells and inhibits phorbol ester-induced protein kinase C (PKC) activity. Reported to inhibit production of inflammatory cytokines by peripheral blood monocytes and alveolar macrophages. Potent inhibitor of EGFR tyrosine kinase and IκB kinase. Inhibits inducible nitric oxide synthase (iNOS), cycloxygenase and lipoxygenase. Easily penetrates into the cytoplasm of cells, accumulating in membranous structures such as plasma membrane, endoplasmic reticulum and nuclear envelope.
References Srinivasan, et al.: J. Pharm. Pharmacol., 5, 448 (1953), Tu, B., et al.: J .Cell Biol., 164, 341 (2004), Xu, G., et al.: Biochemistry, 44, 9817 (2005), Johnson, J., et al.: Cancer Lett., 255, 170 (2007),

Applications Bunazosin Hydrochloride is an α-1 adrenergic receptor antagonist that acts as an anti-cancer and anti-glaucoma drug.
References Daisy, P. et al.: Asian. J. Pharm. Clin. Res., 5, 149 (2012); Sakanaka, K. et al.: Biol. Pharm. Bull., 31, 1590 (2008);