Inhibiteur d’enzymes

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);

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 GDC 0152 is a peptidomimetic small molecule antagonist of inhibitor of apoptosis (IAP) proteins with antitumor activity.
References Yue, Q., et. al.: Drug Metab. Dispos., 41, 508 (2013)

Stability Hygroscopic
Applications 3a,6,7,7a-Tetrahydro-5-(hydroxymethyl)-2-methyl-(3aR,5R,6S,7R,7aR)-5H-pyrano[3,2-d]thiazole-6,7-diol, can be used in the synthesis of Hexosaminidase inhibitors, which are the new drug candidates for the therapy of osteoarthritis.
References Liu, J. et al.: Chem. Bio., 8, 701 (2001);

Applications It is a potent inhibitor of protein kinase C (PKC) activity. Bisindolylmaleimide VIII (Bis VIII) has been previously shown to enhance Fas-mediated apoptosis through a protein kinase C-independent mechanism.
References Emery, J., et al.: J. Biol. Chem., 273, 14363 (1998), Wiley, S., et al.: Immunity, 3, 673 (1995), MacFarlane, M., et al.: Biochem. J., 348, 93 (2000),

Applications A selective inhibitor of protein kinase C or cyclic-nucleotide-dependent protein kinases.
References Hidaka, H. and Kawamoto, S.: Biochem. and Biophys. Res. Comm., 125, 1, 258 (1984)

Stability Moisture Sensitive
Applications An inhibitor of cholinesterase.
References Berman, H., et al.: J. Biol. Chem., 264, 3951 (1989), Millard, C., et al.: Biochemistry, 37, 237 (1998), Koellner, G., et al.: J. Mol. Biol., 296, 713 (2000),

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),

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)

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

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);

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 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 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)