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1-萘羥肟酸

1-萘羥肟酸

中文名稱1-萘羥肟酸
中文同義詞1-萘羥肟酸;Α-萘羥肟酸;1-NAPHTHOHYDROXAMIC ACID,HDAC8抑制劑;1-萘羥肟酸,10 MM DMSO 溶液
英文名稱1-NAPHTHOHYDROXAMIC ACID
英文同義詞Naphthalene-1-carbohydroximic acid;N-Hydroxy-1-naphthalenecarboxamide;a-Naphthohydroxamic acid;NSC 57457;HDAC Inhibitor XIX, Compound 2;N-HYDROXYNAPHTHALENE-1-CARBOXAMIDE;alpha-naphthohydroxamicacid;n-hydroxy-1-naphthalenecarboxamid
CAS號6953-61-3
分子式C11H9NO2
分子量187.19
EINECS號
相關(guān)類別試劑和補(bǔ)充物;標(biāo)準(zhǔn)品;Hydroxylamines;Hydroxylamines (N-Substituted)
Mol文件6953-61-3.mol
結(jié)構(gòu)式1-萘羥肟酸 結(jié)構(gòu)式

1-萘羥肟酸 性質(zhì)

熔點(diǎn)176-178 °C
密度1.291±0.06 g/cm3(Predicted)
儲存條件2-8°C
溶解度二甲基亞砜:≥5mg/mL
形態(tài)白色固體
酸度系數(shù)(pKa)8.91±0.30(Predicted)
顏色白色至棕褐色

1-萘羥肟酸 用途與合成方法

1-Naphthohydroxamic acid (Compound 2) 是一種有效的,選擇性的 HDAC8 抑制劑,IC50 為 14 μM。1-Naphthohydroxamic acid 對 HDAC8 的選擇性高于 I 類 HDAC1 和 II 類 HDAC6 (IC50 >100 μM)。1-Naphthohydroxamic acid 不會增加整體組蛋白 H4 的乙酰化,也不會降低總細(xì)胞內(nèi) HDAC 的活性。1-Naphthohydroxamic acid 可誘導(dǎo)微管蛋白乙酰化。

HDAC8

14 μM (IC 50 )

HDAC1

>100 μM (IC 50 )

HDAC6

>100 μM (IC 50 )

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

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.

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.

Animal Model: NMRI Foxn1 nude mice
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.

安全信息

危險類別碼52
WGK Germany3
RTECS號QJ1894500
海關(guān)編碼2928009090

MSDS信息

更新日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2025/02/08HY-1305381-萘羥肟酸
1-Naphthohydroxamic acid
6953-61-31 mg175元
2025/02/08HY-1305381-萘羥肟酸
1-Naphthohydroxamic acid
6953-61-35mg404元

1-萘羥肟酸 上下游產(chǎn)品信息

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