| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
HPOB is a novel, potent and selective inhibitor of histone deacetylase 6 (HDAC6) with potential anticancer activity. It exhibits >30-fold selectivity for HDAC6 over other HDAC isoforms and inhibits HDAC6 with an IC50 of 56 nM.
| Targets |
HDAC6 ( IC50 = 0.056 μM ); HDAC3/NCOR2 ( IC50 = 1.7 μM ); HDAC8 ( IC50 = 2.8 μM ); HDAC1 ( IC50 = 2.9 μM ); HDAC10 ( IC50 = 3.0 μM ); HDAC2 ( IC50 = 4.4 μM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The fluorogenic release of 7-amino-4-methylcoumarin from substrate upon deacetylase enzymatic activity is used to detect the in vitro activities of the 11 recombinant human zinc-dependent HDAC enzymes. Ten percent DMSO in HDAC assay buffer is used to prepare a series of dilutions of the unique HDAC6 compound, tubacin, and SAHA. Five microliters of each dilution is then added to a 50 microliter reaction, ensuring that the final concentration of DMSO is one percent in each reaction. The enzymatic reactions are carried out in duplicate in a 50-μL mixture containing an HDAC substrate, an HDAC enzyme, an HDAC assay buffer, 5 μg BSA, and a test compound for 30 minutes at 37 °C. Following the enzymatic reactions, 50 μL of 2× HDAC developer is added to every well, and the plate is left to incubate for a further fifteen minutes at room temperature. A Synergy microplate reader is used to measure the fluorescence intensity at an excitation of 360 nm and an emission of 460 nm. The assays include positive controls (SAHA, a known HDAC inhibitor) and negative controls (no enzyme, no inhibitor, or medication with no HDAC inhibition activity). The drug concentration that causes a 50% decrease in HDAC activity when compared to the control is known as the IC50.
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| Cell Assay |
The prescribed doses of HPOB are cultivated in normal (HFS) and transformed (LNCaP, A549, and U87) cells for a duration of 72 hours. A positive control is five micromolars of SAHA. Prism 5 was utilized to construct the graphs.
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| Animal Protocol |
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| References |
| Molecular Formula |
C17H18N2O4
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| Molecular Weight |
314.34
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| Exact Mass |
314.126
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| Elemental Analysis |
C, 64.96; H, 5.77; N, 8.91; O, 20.36
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| CAS # |
1429651-50-2
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| Related CAS # |
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| PubChem CID |
71532921
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| Appearance |
Off-white to pink solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.649
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| LogP |
-0.05
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
23
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| Complexity |
388
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| Defined Atom Stereocenter Count |
0
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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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| InChi Key |
RFAZNTABYJYOAR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18N2O4/c20-11-10-19(15-4-2-1-3-5-15)16(21)12-13-6-8-14(9-7-13)17(22)18-23/h1-9,20,23H,10-12H2,(H,18,22)
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| Chemical Name |
N-hydroxy-4-[2-[N-(2-hydroxyethyl)anilino]-2-oxoethyl]benzamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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