HPOB

Catalog No.S7278 Batch:S727801

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Technical Data

Formula

C17H18N2O4
Molecular Weight 314.34 CAS No. 1429651-50-2
Solubility (25°C)* In vitro DMSO 62 mg/mL (197.23 mM)
Ethanol 38 mg/mL (120.88 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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] View More
56 nM 1.7 μM 2.8 μM 2.9 μM 3.0 μM
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]
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]

Protocol (from reference)

Kinase Assay:[1]
  • 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 Assay:[1]
  • 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.

Animal Study:[1]
  • Animal Models

    Mice bearing CWR22 human prostate cancer xenografts

  • Dosages

    300 mg/kg daily

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Neurochem Int, 2016, 99:239-51.]

Data from [Data independently produced by , , Molecules, 2018, 23(5)]

Selleck's HPOB has been cited by 3 publications

HDAC3 inhibitor RGFP966 controls bacterial growth and modulates macrophage signaling during Mycobacterium tuberculosis infection [ Tuberculosis (Edinb), 2021, 127:102062] PubMed: 33639591
Anti-Proliferative Activity of HPOB against Multiple Myeloma Cells via p21 Transcriptional Activation [Liu L Molecules, 2018, 23(5)] PubMed: 29710846
HPOB, an HDAC6 inhibitor, attenuates corticosterone-induced injury in rat adrenal pheochromocytoma PC12 cells by inhibiting mitochondrial GR translocation and the intrinsic apoptosis pathway [Li ZY, et al. Neurochem Int, 2016, 99:239-51] PubMed: 27522966

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.