Art. -Nr.: HY-19747

HPOB

3 Cited Publications

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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.

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Reinheit: 99.54%
CAS. Nr.: 1429651-50-2
Formel: C₁₇H₁₈N₂O₄
Molecular Weight:314.34

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

HPOB Chemical Structure

CAS. Nr.: 1429651-50-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
697	IC₅₀	8330 nM Compound: HPOB	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	[PMID: 31710483]
HAL-01	IC₅₀	13.86 μM Compound: HPOB	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	[PMID: 38714044]
HAL-01	IC₅₀	13.9 μM Compound: HPOB	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	[PMID: 36351184]
HL-60	IC₅₀	11.3 μM Compound: HPOB	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	[PMID: 36351184]
HL-60	IC₅₀	11.33 μM Compound: HPOB	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	[PMID: 38714044]
Jurkat	IC₅₀	16.07 μM Compound: HPOB	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	[PMID: 38714044]
Jurkat	IC₅₀	16.1 μM Compound: HPOB	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	[PMID: 36351184]
Sf21	IC₅₀	>10 μM Compound: 207	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	[PMID: 30245394]
Sf9	IC₅₀	>10 μM Compound: 207	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	[PMID: 30245394]
Sf9	IC₅₀	>10 μM Compound: 207	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	[PMID: 30245394]
Sf9	IC₅₀	121 nM Compound: HPOB	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	[PMID: 31710483]
Sf9	IC₅₀	2.8 μM Compound: 207	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	[PMID: 30245394]
Sf9	IC₅₀	2100 nM Compound: HPOB	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	[PMID: 31391882]
Sf9	IC₅₀	85 nM Compound: HPOB	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	[PMID: 31391882]

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].

MedChemExpress (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].

MedChemExpress (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.

Chemical Information

CAS. Nr. 1429651-50-2
Appearance Solid
Molecular Weight 314.34
Formel C₁₇H₁₈N₂O₄
Color Off-white to pink
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 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

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.

Protocol 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

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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HPOB

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) HPOB

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HPOB

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) HPOB

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HPOB Related Classifications

HY-19747 Related Classifications