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DNA HDAC inhibitor HDAC enzyme Acetatylated Lysine Histone tetramer HISTONE DEACETYLASE INHIBITORS 1 9

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Chromosome DNA Chromosomes are made up of DNA, the genetic material of the cell. DNA is wrapped around Histone proteins, which can be acetylated or deacetylated depending on the action of enzymes known as Histone Deacetylases (HDACs). 2 9 Histones

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Histone Deacetylases (HDACs) are also known as Lysine Deacetylases (LDACs), since several isoforms are present on the cell cytoplasm, where they exert their action on Lys residues found on proteins other than histones. 3 9 Histones Nucleus HDAC6 Microtubules

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HDAC6 binds to microtubules in the cytoplasm and takes part in several processes, such as unfolded protein elimination via aggresome/proteasome pathway. HDAC6 inhibition is related to cancer cell death and treatment of inflammatory and autoimmune diseases. 4 9 Histones Nucleus HDAC6 Microtubules

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Histones Histone tetramer Acetatylated Lysine HDAC enzyme 5 9 In the absence of an HDAC selective inhibitor, histone proteins become hypocetylated; DNA is tightly wrapped around histone tetramers, and, in general, gene transcription is silenced. Histone hypoacetylation Acetatylated Lysine

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Histone tetramer Acetatylated Lysine HDAC enzyme HDAC inhibitor Histone hyperacetylation 6 9 In the presence of an HDAC selective inhibitor, histone proteins become hyperacetylated; DNA unwrapps from histones, and genes become more accesible to transcription factors. Ikerchem is developping unique and potent isoform selective and pan- HDAC inhibitors.

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Histone hyperacetylation 7 9 When the HDAC isoform that is inhibited with an HDAC inhibitor is localized to the nucleous of the cell, histone hyperacetylation provokes that previously silenced genes are turned on, and others are turned off. Gene regulation is key in multiple oncogenic processes. Gene Transcription ON Gene Transcription OFF

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Gene Transcription ON Gene Transcription OFF 8 9 HDAC inhibitors therefore provoke a change on the expression pattern of our genome, activating the expression of tumor suppresor genes such as p53, and silencing the expresion of oncogenes such as p21.

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8 9 Ikerchem is developping first and best in class isoform selective HDAC inhibitors, as well as improved HDAC pan-inhibitors. Our interest in generating molecules with improved toxicological profiles, makes of our lead molecules excellent drug candidates.

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