Deacetylase(s)

 

Deacetylases, as the name implies, are enzymes that remove acetyl groups from protein substrates. The most well studied deacetylases are histone deacetylases (HDACs). HDACs oppose the effects of histone acetyltransferases (HATs), restoring the positive charge of the histone tail lysine residue. Removal of the acetyl group results in a more tightly compacted, heterochromatin conformation, thereby negatively regulating gene expression. There are four classes of HDAC enzymes. Classes I, II, and IV contain the classic HDAC enzymes, whereas Class III contains the sirtuin enzymes, which require the cofactor NAD+ for their activity.

Like HATs, HDAC activity is often disrupted in cancer and neurological disorders, and therefore, HDACs are an active drug target. Several HDAC inhibitors have received FDA approval as anti-cancer drugs, and dozens more are in clinical trials. However, many of these inhibitors are not specific for particular HDAC isozymes. Complicating matters is the fact that many HDACs exhibit low substrate specificity by themselves and a single enzyme can be capable of deacetylating multiple sites within histones. This makes the task of linking abnormal epigenetic profiles with a specific HDAC very difficult. Careful in vitro and in vivo studies will need to be done to identify the specific HDACs responsible for these abnormalities.

BPS was the first company to offer a full suite of active HDAC and Sirtuin proteins. In addition to high purity enzymes, BPS provides isotype-specific assay kits for screening and profiling, as well as a number of HDAC inhibitors/activators and substrates for all of the HDAC classes.

References:

1.  Barneda-Zahonero, B. et al., Mol. Oncol. 2012; 6: 579-589.
2.  De Ruister, A.J.M., et al., Biochem. J. 2003; 370: 737-749. 

 

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Catalog#SizeProduct NamePrice
50866 50 µl Fluorogenic Sirtuin 6 Substrate
$230
27209 500 µg HC Toxin
$140
50031 20 ml HDAC Assay Buffer
$35
50041 96 reactions HDAC class 2a Fluorogenic Assay Kit
$435
50030 6 ml HDAC developer (2X)
$200
50033 96 reactions HDAC Fluorogenic Assay Kit
$435
50034 96 reactions HDAC Fluorogenic Assay Kit (Green)
$435
50061 96 reactions HDAC1 Fluorogenic Assay Kit
$430
53001 96 reactions HDAC1 Kinetic Assay Kit
$535
50051 50 µg HDAC1, FLAG-tag, His-tag
$425
50058 50 µg HDAC1, His-Tag, FLAG-Tag (Mouse)
$425
50010 50 µg HDAC10, GST-tag, His-tag
$425
50060 50 µg HDAC10, N-FLAG-tag
$410
50021 10 µg HDAC11
$425
50687 96 reactions HDAC11 Fluorogenic Assay Kit
$430
50011 50 µg HDAC11, GST-tag
$425
50062 96 reactions HDAC2 Fluorogenic Assay Kit
$430
53002 96 reactions HDAC2 Kinetic Assay Kit
$535
50052 50 µg HDAC2, FLAG-tag
$425
50002 50 µg HDAC2, His-tag
$425
50073 96 reactions HDAC3 Fluorogenic Assay Kit
$430
53003 96 reactions HDAC3 Kinetic Assay Kit
$535
50003 50 µg HDAC3/NcoR2 Complex, His-tag
$425
50064 96 reactions HDAC4 Fluorogenic Assay Kit
$430
50004 10 µg HDAC4, GST-tag, His-tag
$425

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