HPOB
Based on 3 publication(s) in Google Scholar
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.
- Purity: 99.54%
- CAS No.: 1429651-50-2
- Formula: C17H18N2O4
- Molecular Weight:314.34
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) HPOB
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Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 697 | IC50 |
8330 nM
Compound: HPOB
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Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
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[PMID: 31710483] |
| HAL-01 | IC50 |
13.86 μM
Compound: HPOB
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Cytotoxicity against human HAL-01 cells measured for 72 hrs by celltiter-glo assay
Cytotoxicity against human HAL-01 cells measured for 72 hrs by celltiter-glo assay
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[PMID: 38714044] |
| HAL-01 | IC50 |
13.9 μM
Compound: HPOB
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Cytotoxicity against human HAL-01 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human HAL-01 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 36351184] |
| HL-60 | IC50 |
11.3 μM
Compound: HPOB
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Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 36351184] |
| HL-60 | IC50 |
11.33 μM
Compound: HPOB
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Cytotoxicity against human HL-60 cells measured for 72 hrs by celltiter-glo assay
Cytotoxicity against human HL-60 cells measured for 72 hrs by celltiter-glo assay
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[PMID: 38714044] |
| Jurkat | IC50 |
16.07 μM
Compound: HPOB
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Cytotoxicity against human Jurkat cells measured for 72 hrs by celltiter-glo assay
Cytotoxicity against human Jurkat cells measured for 72 hrs by celltiter-glo assay
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[PMID: 38714044] |
| Jurkat | IC50 |
16.1 μM
Compound: HPOB
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Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 36351184] |
| Sf21 | IC50 |
>10 μM
Compound: 207
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Inhibition of recombinant human N-terminal GST-tagged/C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus infected Sf21 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay
Inhibition of recombinant human N-terminal GST-tagged/C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus infected Sf21 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay
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[PMID: 30245394] |
| Sf9 | IC50 |
>10 μM
Compound: 207
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Inhibition of human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay
Inhibition of human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay
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[PMID: 30245394] |
| Sf9 | IC50 |
>10 μM
Compound: 207
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Inhibition of recombinant full-length human HDAC11 expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay
Inhibition of recombinant full-length human HDAC11 expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay
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[PMID: 30245394] |
| Sf9 | IC50 |
121 nM
Compound: HPOB
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Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
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[PMID: 31710483] |
| Sf9 | IC50 |
2.8 μM
Compound: 207
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Inhibition of recombinant full-length human C-terminal HDAC8 expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay
Inhibition of recombinant full-length human C-terminal HDAC8 expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay
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[PMID: 30245394] |
| Sf9 | IC50 |
2100 nM
Compound: HPOB
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Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based a
Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based a
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[PMID: 31391882] |
| Sf9 | IC50 |
85 nM
Compound: HPOB
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Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based assay
Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based assay
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[PMID: 31391882] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Normal human foreskin fibroblast (HFS), LNCaP, A549, U87 cells
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Concentration:8, 16, or 32 μM
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Incubation Time:72 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice (CWR22 human prostate cancer xenograf)[1]
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Dosage:300 mg/kg
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Administration:I.p.; daily for 18 days
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Result:Combination with SAHA showed significant shrinkage of CWR22 tumors.
Chemical Information
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CAS No. 1429651-50-2
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Appearance Solid
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Molecular Weight 314.34
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Formula C17H18N2O4
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Color Off-white to pink
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SMILES
O=C(N(CCO)C1=CC=CC=C1)CC2=CC=C(C(NO)=O)C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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EMBO J
Acetylation of TIR domains in the TLR4-Mal-MyD88 complex regulates immune responses in sepsis. [Abstract]2024 Nov;43(21):4954-4983. PMID: 39294473 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Solvent & Solubility
DMSO : 50 mg/mL (159.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lee JH et al. Development of a histone deacetylase 6 inhibitor and its biological effects. Proc Natl Acad Sci U S A. 2013 Sep 24;110(39):15704-9. [Content Brief]
[2]. Li ZY et al. HPOB, an HDAC6 inhibitor, attenuates corticosterone-induced injury in rat adrenal pheochromocytoma PC12 cells by inhibiting mitochondrial GR translocation and the intrinsic apoptosis pathway. Neurochem Int. 2016 Oct;99:239-51. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1813 mL | 15.9063 mL | 31.8127 mL | 79.5317 mL |
| 5 mM | 0.6363 mL | 3.1813 mL | 6.3625 mL | 15.9063 mL | |
| 10 mM | 0.3181 mL | 1.5906 mL | 3.1813 mL | 7.9532 mL | |
| 15 mM | 0.2121 mL | 1.0604 mL | 2.1208 mL | 5.3021 mL | |
| 20 mM | 0.1591 mL | 0.7953 mL | 1.5906 mL | 3.9766 mL | |
| 25 mM | 0.1273 mL | 0.6363 mL | 1.2725 mL | 3.1813 mL | |
| 30 mM | 0.1060 mL | 0.5302 mL | 1.0604 mL | 2.6511 mL | |
| 40 mM | 0.0795 mL | 0.3977 mL | 0.7953 mL | 1.9883 mL | |
| 50 mM | 0.0636 mL | 0.3181 mL | 0.6363 mL | 1.5906 mL | |
| 60 mM | 0.0530 mL | 0.2651 mL | 0.5302 mL | 1.3255 mL | |
| 80 mM | 0.0398 mL | 0.1988 mL | 0.3977 mL | 0.9941 mL | |
| 100 mM | 0.0318 mL | 0.1591 mL | 0.3181 mL | 0.7953 mL |
HPOB Related Classifications
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