1-Naphthohydroxamic acid (Compound 2) 是一种有效的，选择性的HDAC8抑制剂，IC50为 14 μM。1-Naphthohydroxamic acid 对HDAC8的选择性高于 I 类 HDAC1 和 II 类 HDAC6 (IC50>100 μM)。1-Naphthohydroxamic acid 不会增加整体组蛋白 H4 的乙酰化，也不会降低总细胞内 HDAC 的活性。1-Naphthohydroxamic acid 可诱导微管蛋白乙酰化。
| 生物活性 | 1-Naphthohydroxamic acid (Compound 2) is a potent and selectiveHDAC8inhibitor with anIC50of 14 μM. 1-Naphthohydroxamic acid is more selectively forHDAC8than class IHDAC1and class IIHDAC6(IC50>100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellularHDACactivity[1][2].1-Naphthohydroxamic acid can induce tubulin acetylation[3]. |
| IC50& Target[1] | HDAC8 14 μM (IC50) | HDAC1 >100 μM (IC50) | HDAC6 >100 μM (IC50) |
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体外研究
(In Vitro) | 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 IC50against 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].
Cell Proliferation Assay[2] | Cell Line: | BE(2)-C, SK-N-BE(2) and SH-SY5Y cells | | Concentration: | 20 μM, 40 μM | | Incubation Time: | 0 hours, 24 hours, 48 hours, 72 hours, 96 hours, and 144 hours | | Result: | Reduced cell numbers in a concentration-dependent manner. |
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体内研究
(In Vivo) | Dose-limiting toxicities (DLTs) of 1-Naphthohydroxamic acid (compound 2; 0-40 mg/kg; intraperitoneal injection; daily; for 10 day; NMRIFoxn1nude mice) include weight loss and signs of liver toxicity, as evidenced by elevated plasma liver enzymes and detection of necrotic areas on histological liver examination. 1-Naphthohydroxamic acid has the maximum tolerable doses at 50 mg/kg per day. At these concentrations, neither body weight nor blood parameters are critically changed[3].
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].
| Animal Model: | NMRIFoxn1nude mice[3] | | Dosage: | 0 mg/kg, 50 mg/kg, 100mg/kg, 200 mg/kg, 300 mg/kg 400 mg/kg | | Administration: | Intraperitoneal injection; daily; for 10 days | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(667.77 mM;Need ultrasonic) 配制储备液 | 1 mM | 5.3422 mL | 26.7108 mL | 53.4217 mL | | 5 mM | 1.0684 mL | 5.3422 mL | 10.6843 mL | | 10 mM | 0.5342 mL | 2.6711 mL | 5.3422 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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