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
27643-2 25 mg RGFP966
$245
27643-3 100 mg RGFP966
$735
27643-1 5 mg RGFP966
$175
27644-2 10 mg Rocilinostat (ACY-1215)
$180
27644-3 50 mg Rocilinostat (ACY-1215)
$360
27644-1 5 mg Rocilinostat (ACY-1215)
$145
27646-1 1 mg Romidepsin (FK228, depsipeptide)
$195
27646-2 5 mg Romidepsin (FK228, depsipeptide)
$405
27006 500 mg SAHA (Vorinostat)
$190
27324 50 mg Salermide
$345
27331 25 mg SB 939
$475
27200 1 mg Scriptaid
$115
50081 96 reactions SIRT1 (Sirtuin1) Fluorogenic Assay Kit
$445
27323 25 mg SIRT1/2 Inhibitor IV
$405
50087 32 reactions SIRT2 (Sirtuin2) Fluorogenic Assay Kit
$700
50088 32 reactions SIRT3 (Sirtuin3) Fluorogenic Assay Kit
$445
50085 96 reactions SIRT5 (Sirtuin5) Fluorogenic Assay Kit
$445
27652-2 25 mg Sirtinol
$280
27652-1 5 mg Sirtinol
$125
50012 100 µg Sirtuin 1 (193-741), GST-tag
$440
50013 100 µg Sirtuin 2, His-tag
$440
50014 100 µg Sirtuin 3, GST-tag
$440
50015 100 µg Sirtuin 4, GST-tag
$440
50016 100 µg Sirtuin 5, GST-tag
$440
50022 96 reactions Sirtuin 6 Fluorogenic Assay Kit
$445

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