Epigenetic events, such as DNA methylation and covalent modification of histones, have been demonstrated to silence the expression of many genes that suppress malignancy. Since the event is reversible, it is an interesting target for intervention with specific inhibitors of DNA methylation and histone deacetylation.
InvivoGen provides two such inhibitors: - 5-AzadCyd, inhibitor of DNA methyltransferases (DNMTs) - Trichostatin A, inhibitor of histone deacetylases (HDACs)
Both inhibitors have been demonstrated to be promising anticancer agents used either separately or in combination.
5-AzadCyd
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Description
5-Aza-2‘-deoxycytidine (5-AzadCyd, decitabine) is a specific inhibitor of DNA methylation. 5-AzaCyD is a prodrug that requires activation via phosphorylation by deoxycytidine kinase. The nucleotide analog is incorporated into DNA, where it produces an irreversible inactivation of DNA methyltransferase. 5-AZA-CdR is an S-phase-specific agent. The demethylation of DNA by this analog in neoplastic cells can lead to the reactivation of silent tumor-suppressor genes, induction of differentiation or senescence, growth inhibition, and loss of clonogenicity. 5-AZA-CdR was demonstrated to be a potent antineoplastic agent against leukemia and tumors in animal models. Preliminary clinical trials of 5-AZA-CdR using different dose-schedules have shown interesting antineoplastic activity in patients with leukemia, myelodysplastic syndrome (MDS), and non-small cell lung cancer (NSCLC).
Formula
Working Concentration: 0.1-10 µM Molecular weight: 228.21 CAS number : 2353-33-5
Contents and Storage
5-AzadCyd is supplied as an off white powder. Product is shipped at room temperature. Store at -20°C. 5-AzadCyd is stable for at least 1 year.
Trichostatin A (TSA) is a potent and specific inhibitor of histone deacetylase (HDAC). HDAC is overexpressed in a variety of cancers and is closely correlated with oncogenic factors. TSA suppresses the activity of HDAC leading to an increase in histone acetylation. This histone acetylation induces an enhancement of the expression of specific genes that elicit extensive cellular morphologic and metabolic changes, such as growth arrest, differentiation and apoptosis. TSA has been shown to induce apoptosis in many cancer cells at submicromolar concentrations with very low toxicity toward normal cells.
Formula
Working Concentration: 100 ng/ml Molecular weight: 302,37 CAS number : 58880-19-6
Contents and Storage
Trichostatin A is supplied as a white powder. Product is shipped at room temperature. Store at -20°C. Trichostatin A is stable for at least 1 year.
Disclaimer: Our products are provided for research purpose only. Commercial applications may require licensing from third parties.
Note that the sequence of available ORFs provided by InvivoGen can differ from a given reference Genbank record due to genetic variations
and/or alternative splicing. Customers should verify that the version of a gene sold by InvivoGen is suitable for the customer needs.
