Antipain is a protease inhibitor isolated from Actinomycetes. Antipain inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations[1][2].
Merbarone is a Type II DNA topoisomerase inhibitor. Merbarone inhibits the catalytic activity of human topoisomerase IIalpha by blocking DNA cleavage. Merbarone induces activation of caspase-activated DNase and excision of chromosomal DNA loops from the n
Epitalon is a synthetic tetrapeptide with anti-aging properties.1,2,3,4 Dietary administration of epitalon (0.00001% w w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.1 Epitalon (1 μg animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.2 It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.3 Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm of cortisol secretion in senescent female M. mulatta monkeys.4References1. Khavinson, V.K., and Myl'nikov, S.V. Effect of epithalone on the age-specific changes in the time course of lipid peroxidation in Drosophila melanogaster. Bull. Exp. Biol. Med. 130(11), 1116-1119 (2000).2. Anisimov, V.N., Khavinson, V.K., Popovich, I.G., et al. Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology 4(4), 193-202 (2003).3. Kossoy, G., Anisimov, V.N., Ben-Hur, H., et al. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H He mice. In Vivo 20(2), 253-257 (2006).4. Khavinson, V., Goncharova, N., and Lapin, B. Synthetic tetrapeptide epitalon restores disturbed neuroendocrine regulation in senescent monkeys. Neuro. Endocrinol. Lett. 22(4), 251-254 (2001). Epitalon is a synthetic tetrapeptide with anti-aging properties.1,2,3,4 Dietary administration of epitalon (0.00001% w w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.1 Epitalon (1 μg animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.2 It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.3 Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm of cortisol secretion in senescent female M. mulatta monkeys.4 References1. Khavinson, V.K., and Myl'nikov, S.V. Effect of epithalone on the age-specific changes in the time course of lipid peroxidation in Drosophila melanogaster. Bull. Exp. Biol. Med. 130(11), 1116-1119 (2000).2. Anisimov, V.N., Khavinson, V.K., Popovich, I.G., et al. Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology 4(4), 193-202 (2003).3. Kossoy, G., Anisimov, V.N., Ben-Hur, H., et al. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H He mice. In Vivo 20(2), 253-257 (2006).4. Khavinson, V., Goncharova, N., and Lapin, B. Synthetic tetrapeptide epitalon restores disturbed neuroendocrine regulation in senescent monkeys. Neuro. Endocrinol. Lett. 22(4), 251-254 (2001).
Methapyrilene fumarate is a histamine H1 antagonist with sedative action used as a hypnotic and in allergies. It is a hepatocarcinogen in sufficiently high doses, inducing mutations through an indirect genotoxic mechanism; e.g., via an oxidative mechanism or interaction with chromosomal proteins.
GNE-8525 is a potent and selective pan-TRK inhibitor. GNE-8525 demonstrated potent antiproliferation activity with IC50 = 0.003 μM. In a tumor xenograft model derived from the KM12 cell line, GNE-8525 demonstrated in vivo antitumor efficacy when administered at ascending doses twice daily (bid) for 14 days in rats. Deregulated kinase activities of tropomyosin receptor kinase (TRK) family members have been shown to be associated with tumorigenesis and poor prognosis in a variety of cancer types. In particular, several chromosomal rearrangements involving TRKA have been reported in colorectal, papillary thyroid, glioblastoma, melanoma, and lung tissue that are believed to be the key oncogenic driver in these tumors.
Alentemol, also known as U-66444B abd alentamol, is a selective dopamine autoreceptor agonist described as an antipsychotic. Chromosomal breakage following treatment of CHO-K1 cells in vitro with U-68,553B is due to induction of undercondensation of heterochromatin.
Streptonigrin is an aminoquinone antitumor and antibacterial antibiotic produced by Streptomyces flocculus. Streptonigrin inhibits β-Catenin Tcf signaling and shows cytotoxicity in β-catenin-activated cells. Streptonigrin induces delayed chromosomal instability involving interstitial telomeric sequences in Chinese hamster ovary cells. Note: Streptonigrin from natural resource is (-)-rotation, has CAS#3930-19-6 and is a R-isomer.