HDAC

Histone deacetylases (HDACs; EC 3.5.1.98) are a class of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid of histones. Inhibitors of this class of enzymes have a long history of use in psychiatry and neurology as mood stabilizers and anti-epileptics. Moreover, Histone deacetylase inhibitors (HDIs) are being studied as an alleviator or treatment for neurodegenerative diseases[1]. Recently, this class of enzymes is emerging as an exciting new class of potential anticancer agents for the treatment of solid and hematological malignancies[2] by inhibiting the proliferation and induction of differentiation and/or apoptosis of tumor cells in culture and in animal models[3]. HDAC inhibition causes acetylated nuclear histones to accumulate in both tumor and normal tissues, providing a surrogate marker for the biological activity of HDAC inhibitors in vivo[4]. HDAC inhibition not only results in acetylation of histones but also transcription factors such as p53, GATA-1 and estrogen receptor-alpha. The functional significance of acetylation of non-histone proteins and the precise mechanisms whereby HDAC inhibitors induce tumor cell growth arrest, differentiation and/or apoptosis are currently the focus of intensive research. Several HDAC inhibitors have shown impressive antitumor activity in vivo with remarkably little toxicity in preclinical studies.


[1] Histone deacetylase inhibitors: possible implications for neurodegenerative disorders. E. Hahnenet al. Expert Opin Investig Drugs. 2008, 17, 169-84.
[2] The Histone Deacetylase Inhibitor LBH589 Is a Potent Antimyeloma Agent that Overcomes Drug Resistance. Maiso P. et al. Cancer Res 2006, 66, 5781.
[3] Use of the Nitrile Oxide Cycloaddition (NOC) Reaction for Molecular Probe Generation: A New Class of Enzyme Selective Histone Deacetylase Inhibitors (HDACIs) Showing Picomolar Activity at HDAC6. AP Kozikowski et al.  J. Med. Chem. 2008, 51, 4370–4373.
[4] Histone deacetylase inhibitors in cancer treatment. Vigushin DM, Coombes RC. Anticancer Drugs. 2002 ,13, 1-13.

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Axon ID Name Description From price
2471 BRD 73954 Dual HDAC 6/8 inhibitor with excellent selectivity over the other HDACs €85.00
2014 CI 994 HDAC inhibitor that causes histone hyperacetylation in living cells €70.00
1645 HDAC6 inhibitor ISOX HDAC6 Inhibitor €105.00
2529 JNJ 26481585 dihydrochloride Potent, orally available second-generation pan-HDAC inhibitor €125.00
1548 LBH 589 HDAC1 Inhibitor €95.00
2430 LW479 HDAC inhibitor with cytotoxicity in a panel of breast cancer cell lines. €135.00
1707 MC 1568 HDAC inhibitor (class IIA selective) €85.00
2505 Mocetinostat Class I selective HDAC inhibitor with broad spectrum antitumor activity €80.00
1803 MS 275 Inhibitor of HDAC (1 and 3 Selective) €80.00
2359 Nexturastat A HDAC6 inhibitor with good selectivity over HDAC1 and HDAC8 €95.00
1853 PCI 34051 HDAC8 Inhibitor €90.00
1801 Pyroxamide HDAC1 Inhibitor €90.00
2195 RGFP 966 HDAC3 specific inhibitor €85.00
2495 Santacruzamate A Picomolar level HDAC2 inhibitor with little inhibition of HDAC4 and HDAC6 €85.00
1777 SB 939 HDAC inhibitor (1, 2, 4 Selective) €105.00

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