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);

Applications Isopteropodine is an alkaloid extract from Uncaria Tomentosathat is believed to possess antiproliferative and pro-apoptotic effects.
References Rinner, B. et al.: Anticancer. Res., 29, 4519 (2009); Cheng, A. et al.: Food Chem. Toxicol., 45, 2206 (2007);

Applications Ceramide-1-phosphate blocks apoptosis through inhibition of acid sphingomyelinase in macrophages.

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 An analogue of Olomoucine (Cat. # O567000) that acts as a potent inhibitor of Cdk 1 (IC50=100nm) and Cdk2 (IC50=80nm). Also displays antiproliferative and proapoptotic effects.
References Wermeulen, K., et al.: Leukemia, 16, 299(2002)

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);

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 (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 20(R)-Ginsenoside Rg3 causes an inhibition of phosphatidylinositol 3-kinase/Akt activation that, in turn, results in modulations in Bcl-2 family proteins in such a way that the apoptosis of U87 cells are regulated. Elicits a significant inhibition of in vitro cell adhesion and invasion of U87 cells. in vitro stereoselective inhibition of ginsenosides toward UDP-glucuronosyltransferase isoforms and in vivo inhibition of tumor angiogenesis of lung cancer.
References Liu, Y., et al.: Chengdu Yixueyuan Xuebao, 9, 4 (2014); Liu, Y., et al.: Linchuang Junyi Zazhi, 42, 1138 (2014), Kim, D., et al.: Toxicol. Lett., 259, 1 92016); Geng, L., et al.: Zhonghua Zhongyiyao Zazhi, 29, 601 (2014)

Applications Graveoline is an apoptosis and autophagy inducer in skin melanoma cancer cells.

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

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

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),

Stability Hygroscopic
Applications Delanzomib is an orally active proteasome inhibitor. Delanzomib has been shown to down-modulate NF-κB, induce apoptosis, inhibit angiogenesis and M-CSF-RANKL-induced osteoclastogenesis.
References Piva, R. et al.: Blood, 111, 2765 (2008); Sanchez, E. et al.: Br. J. Haematol., 148, 569 (2010);

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 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)