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
50041 96 reactions HDAC class 2a Fluorogenic Assay Kit
$405
50033 96 reactions HDAC Fluorogenic Assay Kit
$405
50034 96 reactions HDAC Fluorogenic Assay Kit (Green)
$405
50061 96 reactions HDAC1 Fluorogenic Assay Kit
$405
53001 96 reactions HDAC1 Kinetic Assay Kit
$510
50062 96 reactions HDAC2 Fluorogenic Assay Kit
$405
53002 96 reactions HDAC2 Kinetic Assay Kit
$510
50073 96 reactions HDAC3 Fluorogenic Assay Kit
$405
53003 96 reactions HDAC3 Kinetic Assay Kit
$510
50064 96 reactions HDAC4 Fluorogenic Assay Kit
$405
50065 96 reactions HDAC5 Fluorogenic Assay Kit
$405
50067 96 reactions HDAC7 Fluorogenic Assay Kit
$405
50068 96 reactions HDAC8 Fluorogenic Assay Kit
$405
50069 96 reactions HDAC9 Fluorogenic Assay Kit
$405
50081 96 reactions SIRT1 (Sirtuin1) Fluorogenic Assay Kit
$405
50087 32 reactions SIRT2 (Sirtuin2) Fluorogenic Assay Kit
$650
50088 32 reactions SIRT3 (Sirtuin3) Fluorogenic Assay Kit
$405
50085 96 reactions SIRT5 (Sirtuin5) Fluorogenic Assay Kit
$405
27208 1 mg (S)-HDAC-42
$100
27205 50 mg 4-iodo-SAHA
$110
27228 5 mg AGK2
$135
27329 10 mg Apicidin
$355
27603-2 10 mg AR-42 (OSU-HDAC42)
$230
27603-3 50 mg AR-42 (OSU-HDAC42)
$690
27603-1 5 mg AR-42 (OSU-HDAC42)
$150

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