1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
  2. HDAC
    Apoptosis
  3. HPOB

HPOB 

Cat. No.: HY-19747 Purity: >95.0%
Handling Instructions

HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6.

For research use only. We do not sell to patients.

HPOB Chemical Structure

HPOB Chemical Structure

CAS No. : 1429651-50-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
25 mg USD 192 In-stock
Estimated Time of Arrival: December 31
50 mg USD 288 In-stock
Estimated Time of Arrival: December 31
100 mg USD 468 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 2 publication(s) in Google Scholar

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Description

HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6[1].

IC50 & Target[1]

HDAC6

0.056 μM (IC50)

HDAC3/NCOR2

1.7 μM (IC50)

HDAC8

2.8 μM (IC50)

HDAC1

2.9 μM (IC50)

HDAC10

3.0 μM (IC50)

HDAC2

4.4 μM (IC50)

In Vitro

HPOB (8, 16, or 32 μM; 72 hours) inhibits growth, however, not viability, of normal or transformed cells[1].
In normal (HFS) and transformed (LNCAP, U87, and A549) cells, HPOB causes accumulation of acetylated α-tubulin and acetylated peroxiredoxin, substrates of HDAC6, but not of acetylated histones. HPOB enhances etoposide-, doxorubicin-, and SAHA-induced transformed cell ((LNCAP, U87, and A549 cells) death but not normal cell death[1].
In LNCaP cells cultured with HPOB and etoposide, there was an increase in cleaved PARP, a marker of apoptosis. Combination of HPOB with etoposide increased the accumulation of DNA damage compared with etoposide alone as evidenced by accumulation of γH2AX in LNCaP cells[1].
HPOB attenuates corticosterone-induced injury in rat adrenal pheochromocytoma PC12 cells by inhibiting mitochondrial GR translocation and the intrinsic apoptosis pathway[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Normal human foreskin fibroblast (HFS), LNCaP, A549, U87 cells
Concentration: 8, 16, or 32 μM
Incubation Time: 72 hours
Result: Inhibited cell growth of normal and transformed cells in a concentration-dependent manner but do not induce cell death of normal or transformed cells.
In Vivo

HPOB (300 mg/kg; i.p.; daily for 18 days) and SAHA (50 mg/kg) causes suppression of the growth of established CWR22 tumors[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (CWR22 human prostate cancer xenograf)[1]
Dosage: 300 mg/kg
Administration: I.p.; daily for 18 days
Result: Combination with SAHA showed significant shrinkage of CWR22 tumors.
Molecular Weight

314.34

Formula

C₁₇H₁₈N₂O₄

CAS No.

1429651-50-2

SMILES

O=C(N(CCO)C1=CC=CC=C1)CC2=CC=C(C(NO)=O)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (159.06 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1813 mL 15.9063 mL 31.8127 mL
5 mM 0.6363 mL 3.1813 mL 6.3625 mL
10 mM 0.3181 mL 1.5906 mL 3.1813 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

HPOBHDACApoptosisHistone deacetylasesselectiveanticancerLNCaPA549U87cellsCWR22tumorInhibitorinhibitorinhibit

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HPOB
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