HPOB 1429651-50-2

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Molecular Weight:

314.34 HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.






Biological Activity


In normal (HFS) and transformed (LNCaP, A549, and U87) cells, HPOB
induces acetylation of α-tubulin, however, not histones, and inhibits
cell growth, however, not viability. In HFS cells, HPOB enhances
transformed cell death induced by etoposide, doxorubicin, or SAHA. HPOB
also enhancing etoposide-induced transformed cell death via the
apoptotic pathway in transformed cells.


In mice bearing CWR22 human prostate cancer xenografts, HPOB (300
mg/kg/d i.p.), when in combination with SAHA, causes suppression of the
growth of established tumors, while produces no significant suppression
when used alone.






In Vitro Enzymatic Assay for Histone Deacetylases


In vitro activities of the 11 recombinant human zinc-dependent HDAC
enzymes are detected by fluorigenic release of 7-amino-4-methylcoumarin
from substrate upon deacetylase enzymatic activity. A series of
dilutions of the unique HDAC6 compound, tubacin, and SAHA are prepared
with 10% DMSO in HDAC assay buffer, and 5 μL of the dilution was added
to a 50-μL reaction so that the final concentration of DMSO is 1% in all
of the reactions.


The enzymatic reactions are conducted in duplicate at
37 °C for 30 min in a 50-μL mixture containing HDAC assay buffer, 5 μg
BSA, an HDAC substrate, an HDAC enzyme, and a test compound. After
enzymatic reactions, 50 μL of 2× HDAC developer is added to each well,
and the plate is incubated at room temperature for an additional 15 min.
Fluorescence intensity is measured at an excitation of 360 nm and an
emission of 460 nm using a Synergy microplate reader.


Negative (no
enzyme, no inhibitor, a drug with no HDAC inhibition activity) and
positive controls (known HDAC Inhibitor SAHA) are included in the
assays. IC50 is determined at the drug concentration that results in 50%
reduction of HDAC activity compared with the control.

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Product Categories : Epigenetics > HDAC Inhibitor