Inhibitor Enzymes

Applications 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 Erlotinib (E625000). Selective epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor. Antineoplastic.
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 Moyer, J.D., et al.: Cancer Res., 57, 4838 (1997), Hidalgo, M., et al.: J. Clin. Oncol., 19, 3267 (2001), Perez-Soler, R., et al.: J. Clin. Oncol., 22, 3238 (2004), Blackhall, F.H., et al.: Expert Opin. Pharmacother., 6, 995 (2005),

Applications A derivative of 4-aminopyrazolo[3,4-d]pyridine as tyrosine kinase inhibitor.
References Dohmen, R., et al.: Science, 263, 1273 (1994), Davies, S., et al.: Biochem. J., 351, 95 (2000), Gregan, J., et al.: Mol. Biol. Cell., 14, 3876 (2003), Zeidler, M., et al.: Nat. Biotechnol., 22, 871 (2004), Knight, Z., et al.: Cell, 128, 425 (2007),

Applications (+)-Donepezil is an isomer of Donepezil (D531750), a nootropic, acting as an inhibitor of acetylcholinesterase.
References Ohnishi, A., et al.: J. Clin. Pharmacol., 33, 1086 (1993), Galli, A., et al.: Eur. J. Pharmacol., 270, 189 (1994)

Applications AZD6738 is an orally available morpholino-pyrimidine-based inhibitor of ataxia telangiectasia and rad3 related (ATR) kinase, with potential antineoplastic activity. Upon oral administration, ATR kinase inhibitor AZD6738 selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine/threonine protein kinase CHK1. This prevents ATR-mediated signaling, and results in the inhibition of DNA damage checkpoint activation, disruption of DNA damage repair, and the induction of tumor cell apoptosis. In addition, AZD6738 sensitizes tumor cells to chemo- and radiotherapy. ATR, a serine/threonine protein kinase upregulated in a variety of cancer cell types, plays a key role in DNA repair, cell cycle progression, and survival; it is activated by DNA damage caused during DNA r
References Karnitz, Larry M., et al.: Clin Cancer Res., 21, 4780 (2015); Kwok, Marwan., et al.: Blood., 127, 582 (2016)

Stability Moisture and Temperature Sensitive
Applications An inhibitor of O-GlcNAcase, hexosaminidase A, and hexosaminidase B.
References Baji, H., et al,: Eur. J. Med. Chem., 30, 617 (1995), Vaaje-Kolstad, G., et al.: J. Biol. Chem., 279, 3612 (2004), Perreira, M., et al.: Bioorg. Med. Chem., 14, 837 (2006).

Applications Losartan is a nonpeptide angiotensin II AT1-receptor antagonist. Antihypertensive.
References Chiu, T.A., et al.: J. Pharmacol. Exp. Ther., 252, 711 (1990); McIntyre, M., et al.: Pharmacol. Ther., 74, 181 (1997); Pitt, B., et al.: Lancet, 355, 1582 (2000)