Apoptose

Stability Hygroscopic
Applications A potent and selective ATP-competitive dual inhibitor cdc7/cdk9. It blocks DNA synthesis and affects the phosphorylation of the replicative DNA helicase at Cdc7-dependent phosphorylation sites. Inhibits cell proliferation in a variety of human cell lines and induces apoptosis in a p53-independent manner in vivo. Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK-2).
References Anderson, D.R. et al.: J. Med. Chem., 50, 2647 (2007); Montagnoli, A. et al.: Nature Chem. Biol., 4, 357 (2008); Charych, D.H. et al.: J Cell. Biochem., 104, 1075 (2008); Jackson, P.K. et al.: Nature Chem. Biol., 4, 331 (2008);

Stability Hygroscopic
Applications MelittinTrifluoroacetic Acid Salt is the Trifluoroacetic Acid Salt version of Melittin which is an apoptosis inducer, a NF-κB inhibitor, and a PLA2 activator.
References Han, S., et al.: J Asian Nat Prod Res. 11, 796-804 (2009); Park, C., et al.: Biochem. Biophys. Res. Commun., 394, 170-172 (2010); Park, J.H., et al.: Mol. Cells., 29, 209-215 (2010);

Applications (3S,4S)-(+)-1-Benzyl-3,4-pyrrolidinediol is used as a reagent in organic synthesis including that of pyrrolidine iminocyclitol α-glucosidase inhibitors and (-)-(1R,2R,7S,8aR)-1,2,7-Trihydroxyindolizidine ((-)-7S-OH-Lentiginosine) which has potential proapoptotic properties.
References Guerreiro, L., et al.: Bioorg. Med. Chem., 21, 1911 (2013); Cordero, F., et al.: ChemPlusChem, 77, 224 (2012);

Applications tert-Butyl 4-Bromo-2-fluorobenzoate is an intermediate of enzalutamide (M199800). Enzalutamide is an androgen-receptor antagonist that blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. MDV 3100 has also been shown to induce tumor cell apoptosis, and has no agonist activity. MDV 3100 is a candidate for the treatment of castration-resistant prostate cancer.
References Scher, H.I. et al.: Lancet, 375, 1437 (2010); Bellmunt, J. et al.: Ther. Adv. Med. Oncol., 2, 189 (2010); Ryan, C.J. et al.: J. Clin. Oncol., 29, 3651 (2011);

Applications 2-(4-Chlorophenyl)-4,4-dimethyl-1-cyclohexene-1-carboxaldehyde is an intermediate in various reactions. For example, its an intermediate in preparation of N-​(phenylsulfonyl)​benzamides and N-​(3-​pyridylsulfonyl)​benzamides as apoptosis-​inducing agents for the treatment of cancer and immune diseases and autoimmune diseases.
References Bruncko, M., et al.: PCT Int. Appl. (2010), WO 2010138588 A2 20101202.

Applications Intermediate in the production of cell death regulators and apoptosis promoters.
References Park, C., et al.: J. Med. Chem., 51, 6902 (2008),

Applications Intermediate in the production of cell death regulators and apoptosis promoters.

Applications Monosialoganglioside GM3 can have anti-tumor effects by regulating cell apoptosis, angiogenesis. Monosialoganglioside GM3 can also regulate peripheral insulin receptor signaling and increases in GM3 in adipose tissue of obese humans may contribute to insulin resistance.
References Zhu, Y., et al.: Zhongliu Fangzhi Yanjiu, 42, 450 (2015); Herzer, S., et al.: Diabetes, 64, 3363 (2015); Wentworth, J., et al.: ?Int. J. Obes., 40, 706 (2016)

Applications 4-Methyl-1H-imidazole-5-carboxylic Acid is used in preparation of Cyclohexyl Benzamide compounds for treatment of type II diabetes. Also, used in preparation of Triazolylphenyl substituted Amides as apoptosis signal-regulating kinase inhibitors.
References Hu, Z., et al.: PCT Int. Appl.,(2018); Corkey, B., et al.: U.S., (2015);

Applications (3α,5β,7α,12α,24E)-3,7,12-Trihydroxy-cholest-24-en-26-oic Acid is an intermediate in the synthesis of (25R)-3β,7α,12α-Trihydroxy-5-cholestenoic Acid (T795130), which is an oxysterol, an oxidized derivatives of cholesterol (C432501), which may be important in many biological processes, including cholesterol homeostasis, atherosclerosis, sphingolipid metabolism, platelet aggregation, apoptosis, and protein prenylation,[1] though their roles are poorly understood.
References Schroepfer, G., et al.: Physiol. Rev., 80, 361 (2000); Bjorkhem, I.: J. Clin. Invest., 6, 725(2002); Bjorkhem, I., et al.: Arterio. hromb. Vascul. Biol., 22, 734 (2002)

Applications N-(Ethoxycarbonylmethyl)piperazine is used in the preparation of aralkylpiperazine- and aryl-substituted hydrazines, particularly benzylpiperazineacetyl hydrazones of hydroxyaryl aldehydes, as selective inducers of apoptosis and activators of procaspases for use as anticancer agents.
References Nakagawara, A., et al.: Cancer Res., 57, 4578 (1997), Denault, J., et al.: J. Biol. Chem., 278, 34042 (2003), Traven, A., et al.: Cancer Cell, 5, 107 (2004), Becattini, B., et al.: Chem. Biol., 11, 389 (2004),

Applications Selonsertib is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. Selonsertib interacts with the catalytic kinase domain of ASK1 and prevents its phosphorylation and activation. As a result, the expression of genes involved in fibrosis, cellular proliferation, and apoptosis are down regulated.
References Nelson, C. H. et al.: Clin Pharmacol Ther. 98, 630 (2015); Lin, J. H., et al.: Nephron. 129, 29 (2015)

Applications Pyocyanin is an antibiotic accelerator of neutrophil apoptosis.

Applications Apogossypolone is an anticancer agent that induces apoptosis in carcinoma cells. Antiproliferative.
References Zubair, H. et al.: Eur J. Pharm. Sci., 47, 280 (2012);

Applications Mollugin is an anti-tumor agent inducing apoptosis and autophagy in various cancer models.
References Zhang, L. et al.: Biochem. Biophys. Res. Comm., 450, 247 (2014); Idhayadhulla, A. et al.: Bioorg. Chem., 52, 77 (2014);

L-Cystathionine: nonprotein amino acid; important for sulfur amino acid metabolism; used in cardiovascular research.

Dibenz[a,h]anthracene (CCRIS 208) has induced DNA damage and gene mutations in bacteria and gene mutations and transformation in several types of mammalian cell

Topoisomerase II inhibitor 9: Topo II blocker (IC50: 0.97 μM), DNA intercalator (IC50: 43.51 μM), arrests G2/M in Hep G-2 cells and triggers apoptosis.