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
50060 50 µg HDAC10, N-FLAG-tag
$410
50021 10 µg HDAC11
$425
50687 96 reactions HDAC11 Fluorogenic Assay Kit
$430
50011 50 µg HDAC11, GST-tag
$425
50052 50 µg HDAC2, FLAG-tag
$425
50002 50 µg HDAC2, His-tag
$425
50003 50 µg HDAC3/NcoR2 Complex, His-tag
$425
50004 10 µg HDAC4, GST-tag, His-tag
$425
50045 5 µg HDAC5 (full length), GST-tag
$450
50005 10 µg HDAC5, Catalytic Domain, His-tag
$425
100102 5 µg HDAC5, GST-Tag, His-Tag
$450
50046 50 µg HDAC6 (H216A), GST-tag
$450
50066 50 µg HDAC6 (H611A), GST-tag
$450
50076 96 reactions HDAC6 Fluorogenic Assay Kit
$485
50056 50 µg HDAC6, FLAG-tag
$425
100051 50 µg HDAC6, GST-Tag (HEK293-derived)
$425
50057 50 µg HDAC6, GST-Tag (Mouse)
$425
50006 50 µg HDAC6, GST-tag (Sf9-derived)
$425
50007

5 µg
10 µg
25 µg

HDAC7, GST-tag
Starting at:
$300
50008 50 µg HDAC8, His-tag
$425
50009 10 µg HDAC9, His-tag
$425
27206 10 mg HNHA
$215
27327 10 mg ITF 2357
$310
27632-1 5 mg JNJ-26481585
$230
27632-2 10 mg JNJ-26481585
$295

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