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
27632-2 10 mg JNJ-26481585
$295
27757 20 mg Kaempferol
$110
53029 1 ml Kinetic HDAC Assay Developer
$200
27760-1 10 mg LAQ824 (NVP-LAQ824,Dacinostat)
$250
27760-2 50 mg LAQ824 (NVP-LAQ824,Dacinostat)
$690
27203 5 mg M344
$85
27761-2 25 mg MC1568
$230
27761-1 10 mg MC1568
$135
27019 10 mg Mocetinostat
$150
27011 25 mg MS-275 (Entinostat)
$165
50020 50 µg NcoR2 (SMRT), GST-tag
$410
27326 10 mg Oxamflatin
$455
27201 1 mg Oxamflatin
$105
27020 5 mg Panobinostat
$150
27768-2 50 mg Parthenolide
$100
27768-1 250 mg Parthenolide
$235
27316 50 mg PCI 34051
$490
27769-3 5 mg PCI-24781 (CRA-024781)
$175
27769-1 10 mg PCI-24781 (CRA-024781)
$250
27769-2 50 mg PCI-24781 (CRA-024781)
$690
50063 20 µg pf-HDAC1, Malaria, His-tag, FLAG-tag
$425
27771-2 5 mg Pracinostat (SB939)
$200
27771-3 50 mg Pracinostat (SB939)
$620
27771-1 10 mg Pracinostat (SB939)
$295
27328 50 mg Pyroxamide
$355

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