DISCOVER Bioactive Small Molecules for Gene Regulation

The loss of regulation of gene expression is a key component to many human disease states, including neurodegenerative disorders, autoimmune conditions and, most prominently, cancers. Regulation of gene expression can occur at any point during the transcription of DNA to RNA, the translation of RNA into protein, or through post-translational modifications of a protein. Cell-permeable small-molecule modulators have become a valuable tool in the investigation of gene and protein functions, allowing researchers to target and selectively modify gene expression. Sigma® Life Science understands that in research, it is essential to ensure your target is the right target. Sigma offers a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

An active area of gene regulation research is that of epigenetics. Epigenetic modifications are stable, but potentially reversible alterations in gene expression that occur without permanent changes in the DNA sequence but can still be passed on from generation to generation. Well studied epigenetic processes include post-translational modification (e.g. methylation, acetylation) of chromatin-associated proteins, mainly histone proteins, and DNA methylation. The discovery of small molecule regulators (activators or inhibitors) of epigenetic modification enzymes provides researchers with tools with which to investigate the biological consequences of chromatin modifications. In addition to a variety of small molecule regulators for epigenetic targets, Sigma provides novel chemical probes for epigenetics research through a partnership with the Structural Genomics Consortium (SGC). These well-characterized probes potently and selectively inhibit the activity of proteins involved in epigenetic control, including well-studied targets such as the bromodomain-containing BET family of proteins and histone methyltransferases. Visit to learn more about the epigenetic probes from the SGC.

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