Home Cytoskeletal Signaling HDAC inhibitor HPOB For research use only.

HPOB

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

HPOB Chemical Structure

HPOB Chemical Structure

CAS No. 1429651-50-2

Purity & Quality Control

HPOB Related Products

Signaling Pathway

HDAC Signaling Pathways

HDAC Signaling Pathway

Biological Activity

Description HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.
Targets
HDAC6 [1] HDAC3 [1] HDAC8 [1] HDAC1 [1] HDAC10 [1] Click to View More Targets
56 nM 1.7 μM 2.8 μM 2.9 μM 3.0 μM
In vitro
In vitro 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. [1]
Kinase Assay 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.
Cell Research Cell lines HFS, A549, LNCaP, and U87 cells
Concentrations ~32 μM
Incubation Time 72 hours
Method Normal (HFS) and transformed (LNCaP, A549, and U87) cells are cultured with indicated doses of HPOB for 72 h. Five micromolars SAHA is a positive control.Graphs were constructed using Prism 5.
In Vivo
In vivo 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. [1]
Animal Research Animal Models Mice bearing CWR22 human prostate cancer xenografts
Dosages 300 mg/kg daily
Administration i.p.

Chemical Information & Solubility

Molecular Weight 314.34 Formula

C17H18N2O4
CAS No. 1429651-50-2 SDF Download HPOB SDF
Smiles C1=CC=C(C=C1)N(CCO)C(=O)CC2=CC=C(C=C2)C(=O)NO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 62 mg/mL ( (197.23 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 38 mg/mL

Water : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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