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
27205 50 mg 4-iodo-SAHA
$155
27228 5 mg AGK2
$165
27329 10 mg Apicidin
$365
27603-1 5 mg AR-42 (OSU-HDAC42)
$180
27603-2 10 mg AR-42 (OSU-HDAC42)
$280
27603-3 50 mg AR-42 (OSU-HDAC42)
$710
27608-3 100 mg Belinostat (PXD101)
$445
27608-1 10 mg Belinostat (PXD101)
$140
27608-2 50 mg Belinostat (PXD101)
$305
27204 5 mg CBHA
$150
27202 1 mg Chidamide
$120
27021 50 mg CI-994
$155
27616-2 10 mg CUDC-907
$305
27616-3 50 mg CUDC-907
$705
27616-1 5 mg CUDC-907
$235
27620-2 25 mg Droxinostat
$240
27620-1 10 mg Droxinostat
$155
27103 1 mg EX527
$185
50040 250 nmole Fluorogenic HDAC class 2a substrate
$235
50042 250 nmole Fluorogenic HDAC class 2a substrate 2 (green)
$235
50032 500 nmole Fluorogenic HDAC substrate 1
$235
50038 250 nmole Fluorogenic HDAC Substrate 2 (Green fluorescence)
$235
50037 250 nmole Fluorogenic HDAC substrate 3
$235
50080 500 nmole Fluorogenic SIRT substrate 1
$235
50126 250 nmole Fluorogenic Sirtuin 5 Substrate
$235

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