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
27608-3 100 mg Belinostat (PXD101)
$430
27608-1 10 mg Belinostat (PXD101)
$135
27204 5 mg CBHA
$145
27202 1 mg Chidamide
$115
27021 50 mg CI-994
$150
27616-1 5 mg CUDC-907
$230
27616-2 10 mg CUDC-907
$295
27616-3 50 mg CUDC-907
$685
27620-1 10 mg Droxinostat
$150
27620-2 25 mg Droxinostat
$230
27103 1 mg EX527
$180
50040 250 nmole Fluorogenic HDAC class 2a substrate
$230
50042 250 nmole Fluorogenic HDAC class 2a substrate 2 (green)
$230
50032 500 nmole Fluorogenic HDAC substrate 1
$230
50038 250 nmole Fluorogenic HDAC Substrate 2 (Green fluorescence)
$230
50037 250 nmole Fluorogenic HDAC substrate 3
$230
50080 500 nmole Fluorogenic SIRT substrate 1
$230
50126 250 nmole Fluorogenic Sirtuin 5 Substrate
$230
50866 50 µl Fluorogenic Sirtuin 6 Substrate
$230
27209 500 µg HC Toxin
$140
50031 20 ml HDAC Assay Buffer
$35
50030 6 ml HDAC developer (2X)
$200
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

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