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Histone Acetyltransferases (HATs; also known as Lysine Aceyltransferases or KATs) are a family of enzymes that catalyze the acetylation of lysine residues on histone protein tails. This post-translational modification involves the transfer of an acetyl group from acetyl CoA to form ε-N-acetyl lysine.
|Cat. No.||Product Name / Activity|
|Potent and selective p300/CBP inhibitor; orally bioavailable|
|Noncompetitive PCAF/p300 inhibitor|
|Selective p300/CBP inhibitor|
|Reversible and non-competitive CBP/p300 inhibitor|
|Dual CBP/p300 and BRD4 bromodomain inhibitor|
|Selective p300 inhibitor|
|Inhibitor of KAT5 (Tip60)|
|Steroid receptor coactivator 3 (SRC-3) inhibitor|
|High affinity KAT6A (MOZ) competitive inhibitor|
|Cat. No.||Product Name / Activity|
|Selective CBP/p300 BRD inhibitor|
|Potent CBP/p300 BRD inhibitor|
Histone Acetyltransferases (HATs, KATs) are a family of enzymes that catalyze the acetylation of lysine residues on histone protein tails. This post-translational modification involves the transfer of an acetyl group from acetyl CoA to form ε-N-acetyl lysine. The reverse reaction is carried out by histone deacetylases (HDACs).
Acetylation of key lysine residues on histone proteins is an important epigenetic regulator of chromatin architecture, and therefore gene transcription. Histone acetylation levels have been associated with an open chromatin structure, yet specific marks - including acetylated histone H4 lysine 16 (H4K19) - have been linked to chromatin condensation. Since chromatin architecture directly regulates transcriptional activation, both histone acetylation and histone deacetylation have major influences on the control of cell fate. As a result, dysregulation of chromatin acetylation has been linked to the development of cancer and inflammation.
In addition to altering DNA accessibility, histone acetylation also facilitates the recruitment of bromodomain-containing proteins. Bromodomains are highly conserved protein interaction modules, found in many chromatin remodeling proteins, which recognize and bind to ε-N-acetyl lysine motifs. If histone acetyltransferases are the "writers" of acetylated lysine motifs, and histone deacetylases are the "erasers", bromodomains can be considered to be the "readers" of these epigenetic marks.
Tocris offers the following scientific literature for Histone Acetyltransferases to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
|Gene||Species||Gene Symbol||Gene Accession No.||Protein Accession No.|
|Histone acetyltransferase 1||Human||HAT1||NM_003642||O14929|
|K(lysine) acetyltransferase 2A||Human||KAT2A||NM_021078||Q92830|
|K(lysine) acetyltransferase 2B||Human||KAT2B||NM_003884||Q92831|
|K(lysine) acetyltransferase 5||Human||KAT5||NM_006388||Q92993|
|K(lysine) acetyltransferase 6A||Human||KAT6A||NM_006766||Q92794|
|K(lysine) acetyltransferase 6B||Human||KAT6B||NM_012330||Q8WYB5|
|K(lysine) acetyltransferase 7||Human||KAT7||NM_007067||Q95251|
|K(lysine) acetyltransferase 8||Human||KAT8||NM_032188||Q9H7Z6|
|Clock homolog (mouse)||Human||CLOCK||NM_004898||O15516|
|CREB binding protein||Human||CREBBP||NM_004380||Q92793|
|E1A binding protein p300||Human||EP300||NM_001429||Q09472|
|General transcription factor IIIC, polypeptide 4, 90kDa||Human||GTF3C4||NM_012204||Q9UKN8|
|Nuclear receptor coactivator 1||Human||NCOA1||NM_147223||Q15788|
|Nuclear receptor coactivator 2||Human||NCOA2||NM_006540||Q15596|
|Nuclear receptor coactivator 3||Human||NCOA3||NM_006534||Q9Y6Q9|
|Retinoblastoma binding protein 7||Human||RBBP7||NM_002893||Q16576|
|TAF1 RNA polymerase II, TAT box binding protein (TBP)-associated factor, 250kDa||Human||TAF1||NM_004606||P21675|