1-萘羟肟酸
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- CAS号:
- 6953-61-3
- 英文名:
- 1-NAPHTHOHYDROXAMIC ACID
- 英文别名:
- NSC 57457;Naphthohydroxamicacid;a-Naphthohydroxamic acid;1-NAPHTHOHYDROXAMIC ACID;1-NaphthohydroxamicAcid>alpha-naphthohydroxamicacid;1-NAPHTHOHYDROXAMIC ACID 98+%;HDAC Inhibitor XIX, Compound 2;n-hydroxy-1-naphthalenecarboxamid;1-Naphthalenecarbohydroximic acid
- 中文名:
- 1-萘羟肟酸
- 中文别名:
- Α-萘羟肟酸;1-萘羟肟酸
- CBNumber:
- CB2462406
- 分子式:
- C11H9NO2
- 分子量:
- 187.19
- MOL File:
- 6953-61-3.mol
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1-萘羟肟酸化学性质
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熔点:
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176-178 °C
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密度:
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1.291±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: ≥5mg/mL
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形态:
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White solid
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酸度系数(pKa):
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8.91±0.30(Predicted)
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颜色:
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white to tan
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1-萘羟肟酸性质、用途与生产工艺
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。
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HDAC8
14 μM (IC
50
)
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HDAC1
>100 μM (IC
50
)
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HDAC6
>100 μM (IC
50
)
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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.
1-Naphthohydroxamic acid (compound 2) at concentrations in the range of its in vitro IC
50
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.
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.
Cell Proliferation Assay
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Cell Line:
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BE(2)-C, SK-N-BE(2) and SH-SY5Y cells
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Concentration:
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20 µM, 40 µM
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Incubation Time:
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0 hours, 24 hours, 48 hours, 72 hours, 96 hours, and 144 hours
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Result:
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Reduced cell numbers in a concentration-dependent manner.
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Dose-limiting toxicities (DLTs) of 1-Naphthohydroxamic acid (compound 2; 0-40 mg/kg; intraperitoneal injection; daily; for 10 day; NMRI
Foxn1
nude 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.
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.
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Animal Model:
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NMRI
Foxn1
nude mice
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Dosage:
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0 mg/kg, 50 mg/kg, 100mg/kg, 200 mg/kg, 300 mg/kg 400 mg/kg
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Administration:
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Intraperitoneal injection; daily; for 10 days
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Result:
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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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1-萘羟肟酸
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-130538 | 1-萘羟肟酸
1-Naphthohydroxamic acid | 6953-61-3 | 5mg | 650元 |
| 2024/04/30 | HY-130538 | 1-萘羟肟酸
1-Naphthohydroxamic acid | 6953-61-3 | 10mM * 1mLin DMSO | 720元 |
1-萘羟肟酸
生产厂家
全球有 72家供应商
1-萘羟肟酸国内生产厂家
6953-61-3, 1-萘羟肟酸 相关搜索:
- Hydroxylamines (N-Substituted)
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- Α-萘羟肟酸
- 1-萘羟肟酸
- 6953-61-3
- 1-Naphthalenecarboxamide, N-hydroxy-
- tubulin,anti-proliferation,deacetylate,HDAC8,Inhibitor,1 Naphthohydroxamic acid,hyperacetylated,1Naphthohydroxamic acid,acetylation,inhibit,clone,HDAC,Histone deacetylases,1-Naphthohydroxamic acid
- 1-NaphthohydroxamicAcid>
- HDAC Inhibitor XIX, Compound 2 - CAS 6953-61-3 - Calbiochem
- 1-Naphthalenecarbohydroximic acid
- 1-NAPHTHOHYDROXAMIC ACID 98+%
- Naphthohydroxamicacid
- 1-NAPHTHOHYDROXAMIC ACID
- n-hydroxy-1-naphthalenecarboxamid
- alpha-naphthohydroxamicacid
- N-HYDROXYNAPHTHALENE-1-CARBOXAMIDE
- HDAC Inhibitor XIX, Compound 2
- NSC 57457
- a-Naphthohydroxamic acid
- N-Hydroxy-1-naphthalenecarboxamide
- Naphthalene-1-carbohydroximic acid