Enzimas inhibidoras

Applications Labelled Atorvastatin intermediate as inhibitor of MAP kinase and/or HMG-CoA reductase for the treatment of inflammation.
References Boyd, R., et al.: J. Clin. Pharmacol., 40, 91, (2000), Bogman, K., et al.: Br. J. Pharmacol., 132, 1183 (2001), Backman, J., et al.: Clin. Pharmacol. Ther., 72, 685 (2002), Kalvass, J., et al.: Drug Metab. Dispos., 35, 455 (2007),

Applications A selective HIV protease inhibitor. An analogue of Ritonavir.
References Adkins, J.C., et al.: Drugs, 55, 837 (1998)

Applications Anidulafungin, is a semisynthetic echinocandin that inhibits glucan synthase, an enzyme important in the formation of (1→3)-β-D-glucan, a major fungal cell wall component, and thus is used as antifungal drug.
References Denning, D. W., et al.: J. Antimicrob. Chemother, 40, 611 (1997); Vazquez, J. A., et al.: Clin. Ther., 27(6), 657 (2005);

Impurity Imatinib EP Impurity F
Applications N-(5-Amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidineamine (Imatinib EP Impurity F) is a selective inhibitor of protein kinase C (PKC). It is a COVID19-related research product.
References Szczylik, C., et al.: Science, 253, 562 (1991), Geissler, J., et al.: Cancer Res., 52, 4492 (1992), Paul, R., et al.: J. Med. Chem., 36, 2716 (1993),

Applications Studies have shown compounds of this nature are of pharmacological interest. Also has been shown to inhibit the growth of plants.

Applications An inhibitor of NADPH oxidase (an enzyme responsible for reactive oxygen species production) and is useful in the treatment of various inflammatory diseases.
References Imnpellizzeri, D. et al.: Biochem. Pharmac., 81, 636 (2011); Genovese, T. et al: Brain Res., 1372;

Applications Labelled Dapivirine (D185500). Non-nucleoside Reverse Transcriptase inhibitor. An antiviral agent.
References Qin, B., et al.: J. Med. Chem., 53, 4906 (2010), Woolfson, A., et al.: Int. J. Pharm., 388, 136 (2010), Johnson, T., et al.: Eur. J. Pharm. Sci., 39, 203 (2010),

Applications Atazanavir is a novel azapeptide HIV protease inhibitor (PI). Antiviral.
References Palella, F.J. Jr., et al.: N. Engl. J. Med., 338(13), 853 (1998), Nolan, D., et al.: Drugs, 63(23), 2555 (2003), Musial, B.L., et al.: Am. J. Health Syst. Pharm., 61, 1365 (2004), Wood, R., et al.: J. Acquir. Immune Defic. Syndr., 36, 684 (2004),

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 Labelled Azacytidine (A796000), a potent growth inhibitor and cytotoxic agent. It acts as a demethylating agent by inhibiting DNA methyltransferase.
References Kusaba, H., et al.: Eur. J. Biochem., 262, 924 (1999), Broday, L., et al.: Mol. Cell Biol., 19, 3198 (1999), Qian, X., et al.: Am. J. Pathol., 153, 1475 (1999), Canova, C., et al.: Mech. Ageing Dev., 101, 153 (1998)

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. Biol. Chem., 264, 9, 4924 (1989)

Applications Isotope labelled Dolutegravir is a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir is currently in Phase III clinical trials for the treatment of HIV infection. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.
References Kobayashi, M. et al. Antimicrob Agents Chemother., 55, 813 (2011); Garrido, C. et al.: Antiviral, Res., 90, 164 (2011); Lenz, J.C.C. et al.: Exp. Opin. Invest. Drugs, 20, 537 (2011);

Applications Labelled Dutasteride (D735000). Dutasteride is a dual inhibitor of 5α-reductase isoenzymes type 1 and 2; structurally related to Finasteride (F342000). Dutasteride is used in the treatment of benign prostatic hyperplasia.
References Bakshi, R.K., et al.: J. Med. Chem., 38, 3189 (1995), Gisleskog, P.O., et al.: Brit. J. Clin. Pharmacol., 47, 53 (1999), Djavan, B., et al.: Expert Opin. Pharmacother., 6, 311 (2005),

Applications A nonsteroidal estrogen antagonist.
References Gladek, A., et al.: J. Biol. Chem., 264, 16847 (1989), Han, X., et al.: Cancer Res., 52, 1360 (1992), Williams, G., et al.: Carcinogenesis, 14, 315 (1993),Coradini, D., et al.: Anticancer Res., 14, 1059 (1994),

Applications A 5-HT3 receptor antagonist. Used as an antiemetic.
References Sato, N., et al.: Japan J. Pharmacol., 59, 443 (1992), Haga, K., et al.: Japan J. Pharmacol., 63, 377 (1993)

Applications A labelled DNA topoisomerase II inhibitor. Semi-synthetic derivative of podophyllotoxin, related structurally to Teniposide. Antineoplastic.
References Burden, D.A., et al.: J. Biol. Chem., 271, 29238 (1996), Joel, S., et al.: Cancer Treat. Rev., 22, 179 (1996),