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
27642-3 500 mg Resveratrol
$170
27643-2 25 mg RGFP966
$240
27643-3 100 mg RGFP966
$715
27643-1 5 mg RGFP966
$170
27644-2 10 mg Rocilinostat (ACY-1215)
$175
27644-3 50 mg Rocilinostat (ACY-1215)
$350
27644-1 5 mg Rocilinostat (ACY-1215)
$140
27646-1 1 mg Romidepsin (FK228, depsipeptide)
$190
27646-2 5 mg Romidepsin (FK228, depsipeptide)
$395
27006 500 mg SAHA (Vorinostat)
$185
27324 50 mg Salermide
$335
27331 25 mg SB 939
$460
27200 1 mg Scriptaid
$110
27323 25 mg SIRT1/2 Inhibitor IV
$395
27652-2 25 mg Sirtinol
$270
27652-1 5 mg Sirtinol
$120
50012 100 µg Sirtuin 1 (193-741), GST-tag
$425
50013 100 µg Sirtuin 2, His-tag
$425
50014 100 µg Sirtuin 3, GST-tag
$425
50015 100 µg Sirtuin 4, GST-tag
$425
50016 100 µg Sirtuin 5, GST-tag
$425
50022 96 reactions Sirtuin 6 Fluorogenic Assay Kit
$430
50017 100 µg Sirtuin 6, GST-tag
$425
50018 100 µg Sirtuin 7, FLAG-tag
$425
50090 20 ml Sirtuin Assay Buffer
$35

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