Histone Deacetylases

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 Bioscience 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.

Assay Kits
HDAC
HDAC5
HDAC Assay Buffer
SIRT5 (Sirtuin5)
HDAC1
HDAC6
HDAC developer (2X)
Sirtuin Assay Buffer
HDAC2
HDAC7
SIRT1 (Sirtuin1)
Sirtuin Developer (2X)
HDAC3
HDAC8
SIRT2 (Sirtuin2)
 
HDAC4
HDAC9
SIRT3 (Sirtuin3)
 

Enzymes
HDAC1
HDAC6
HDAC11
Sirtuin 4
HDAC2
HDAC7
NcoR2 (SMRT)
Sirtuin 5
HDAC3
HDAC8
Sirtuin 1
Sirtuin 6
HDAC4
HDAC9
Sirtuin 2
Sirtuin 7
HDAC5
HDAC10
Sirtuin 3
 

Substrates 
Fluorogenic HDAC class 2a substrate
Fluorogenic HDAC substrate 3
Fluorogenic HDAC class 2a substrate 2 (green)
Fluorogenic SIRT substrate 1
Fluorogenic HDAC substrate 1
Fluorogenic Sirtuin 5 Substrate
Fluorogenic HDAC Substrate 2 (Green fluorescence) 

Inhibitors / Activators
(S)-HDAC-42LAQ824 (NVP-LAQ824,Dacinostat)Salermide
4-iodo-SAHAM344SB 939
AGK2MC1568Scriptaid
ApicidinMocetinostatSIRT1/2 Inhibitor IV
AR-42 (OSU-HDAC42)MS-275 (Entinostat)Sirtinol
Belinostat (PXD101)OxamflatinSodium Phenylbutyrate
CBHAPanobinostatSplitomicin
ChidamideParthenolideSRT1720
CI-994PCI 34051Suberohydroxamic Acid (SBHA)
CUDC-101PCI-24781 (CRA-024781)Tenovin-1
CUDC-907Pracinostat (SB939)Tenovin-6
DroxinostatPyroxamideTrichostatin A (TSA)
EX527Resminostat (RAS2410)Tubacin
HC ToxinResveratrolTubastatin A
HNHARGFP966Tubastatin A hydrochloride
ITF 2357Rocilinostat (ACY-1215)Valproic Acid
JNJ-26481585Romidepsin (FK228, depsipeptide)
KaempferolSAHA (Vorinostat)



Source:
Website: BPS Bioscience

Related to:
Brands: BPS Bioscience