1-Naphthohydroxamic acid
Based on 2 publication(s) in Google Scholar
1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity.1-Naphthohydroxamic acid can induce tubulin acetylation.
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- 純度: 99.59%
- CAS 番号: 6953-61-3
- 分子式: C11H9NO2
- 分子量:187.19
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 1-Naphthohydroxamic acid
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生物活性
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HDAC8 14 μM (IC50) |
HDAC1 >100 μM (IC50) |
HDAC6 >100 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RBL-1 | IC50 |
43 μM
Compound: 22
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In vitro inhibitory activity against 5-lipoxygenase in rat basophilic leukemia cells(RBL-1)
In vitro inhibitory activity against 5-lipoxygenase in rat basophilic leukemia cells(RBL-1)
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[PMID: 2308149] |
| RBL-1 | IC50 |
43 μM
Compound: 8
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In vitro inhibitory activity against RBL-1 5-LO
In vitro inhibitory activity against RBL-1 5-LO
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[PMID: 3820229] |
1-Naphthohydroxamic acid (compound 2; 20-40 μM; 0-144 ?hours; BE(2)-C, SK-N-BE(2) and SH-SY5Y cells) treatment reduces cell numbers in a concentration-dependent manner[2].
1-Naphthohydroxamic acid (compound 2) at concentrations in the range of its in vitro IC50 against HDAC8 results in reduced cell density and outgrowth of neurite-like structures that stained positive for neurofilament.1-Naphthohydroxamic acid reduces the formation of clones in soft-agar concentration dependently[2].
When either cell type (HeLa and HEK293 cells) is treated with 1-Naphthohydroxamic acid (compound 2; 0.8 μM, 4 μM, 20 μM or 100 μM), only tubulin becomes hyperacetylated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BE(2)-C, SK-N-BE(2) and SH-SY5Y cells
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Concentration:20 µM, 40 µM
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Incubation Time:0 hours, 24 hours, 48 hours, 72 hours, 96 hours, and 144 hours
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Result:Reduced cell numbers in a concentration-dependent manner.
Pharmacokinetic studies after intraperitoneal administration of the inhibitors identified the half-life of 1-Naphthohydroxamic acid to be ~15?min, with a plasma peak concentration of ~30?μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRI Foxn1 nude mice[3]
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Dosage:0 mg/kg, 50 mg/kg, 100mg/kg, 200 mg/kg, 300 mg/kg 400 mg/kg
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Administration:Intraperitoneal injection; daily; for 10 days
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Result:Dose-limiting toxicities (DLTs) included weight loss and signs of liver toxicity, as evidenced by elevated plasma liver enzymes and detection of necrotic areas on histological liver examination.
化学情報
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CAS 番号 6953-61-3
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性状 Solid
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分子量 187.19
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分子式 C11H9NO2
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Color White to off-white
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SMILES
O=C(C1=C2C=CC=CC2=CC=C1)NO
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別名
1-ナフトヒドロキサム酸; N-ヒドロキシナフタレン-1-カルボキシアミド
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Hypoxia-induced conversion of sensory Schwann cells into repair cells is regulated by HDAC8. [Abstract]2025 Jan 9;16(1):515. PMID: 39779705 -
溶剤 & 溶解度
DMSO : 125 mg/mL (667.77 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (280 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Krennhrubec K, et al. Design and evaluation of 'Linkerless' hydroxamic acids as selective HDAC8 inhibitors. Bioorg Med Chem Lett. 2007 May 15;17(10):2874-8. [Content Brief]
[2]. Oehme I, et al. Histone deacetylase 8 in neuroblastoma tumorigenesis. Clin Cancer Res. 2009 Jan 1;15(1):91-9. [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 | 5.3422 mL | 26.7108 mL | 53.4217 mL | 133.5541 mL |
| 5 mM | 1.0684 mL | 5.3422 mL | 10.6843 mL | 26.7108 mL | |
| 10 mM | 0.5342 mL | 2.6711 mL | 5.3422 mL | 13.3554 mL | |
| 15 mM | 0.3561 mL | 1.7807 mL | 3.5614 mL | 8.9036 mL | |
| 20 mM | 0.2671 mL | 1.3355 mL | 2.6711 mL | 6.6777 mL | |
| 25 mM | 0.2137 mL | 1.0684 mL | 2.1369 mL | 5.3422 mL | |
| 30 mM | 0.1781 mL | 0.8904 mL | 1.7807 mL | 4.4518 mL | |
| 40 mM | 0.1336 mL | 0.6678 mL | 1.3355 mL | 3.3389 mL | |
| 50 mM | 0.1068 mL | 0.5342 mL | 1.0684 mL | 2.6711 mL | |
| 60 mM | 0.0890 mL | 0.4452 mL | 0.8904 mL | 2.2259 mL | |
| 80 mM | 0.0668 mL | 0.3339 mL | 0.6678 mL | 1.6694 mL | |
| 100 mM | 0.0534 mL | 0.2671 mL | 0.5342 mL | 1.3355 mL |
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