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. 

 

Items 76 to 100 of 148 total

per page
Page:
  1. 2
  2. 3
  3. 4
  4. 5
  5. 6

Catalog#SizeProduct NamePrice
27760-1 10 mg LAQ824 (NVP-LAQ824,Dacinostat)
$260
11128 20 µg LpxC (E. coli)
$440
27203 5 mg M344
$130
27761-2 25 mg MC1568
$195
27761-1 10 mg MC1568
$140
27019 10 mg Mocetinostat
$120
27011 25 mg MS-275 (Entinostat)
$170
50020 50 µg NcoR2 (SMRT), GST-tag
$420
27326 10 mg Oxamflatin
$470
27201 1 mg Oxamflatin
$150
27020 10 mg Panobinostat
$120
27768-2 50 mg Parthenolide
$125
27768-1 250 mg Parthenolide
$240
27316 50 mg PCI 34051
$505
27769-3 5 mg PCI-24781 (CRA-024781)
$180
27769-1 10 mg PCI-24781 (CRA-024781)
$230
27769-2 50 mg PCI-24781 (CRA-024781)
$495
50063 20 µg pf-HDAC1, Malaria, His-tag, FLAG-tag
$440
27771-2 5 mg Pracinostat (SB939)
$190
27771-3 50 mg Pracinostat (SB939)
$700
27771-1 10 mg Pracinostat (SB939)
$275
27328 50 mg Pyroxamide
$365
27773-2 50 mg Resminostat (RAS2410)
$590
27773-1 10 mg Resminostat (RAS2410)
$260
27642-3 500 mg Resveratrol
$175

Items 76 to 100 of 148 total

per page
Page:
  1. 2
  2. 3
  3. 4
  4. 5
  5. 6