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6953-61-3

中文名稱(chēng) 1-萘羥肟酸
英文名稱(chēng) 1-NAPHTHOHYDROXAMIC ACID
CAS 6953-61-3
分子式 C11H9NO2
分子量 187.19
MOL 文件 6953-61-3.mol
更新日期 2023/03/20 15:41:25
6953-61-3 結(jié)構(gòu)式 6953-61-3 結(jié)構(gòu)式

基本信息

中文別名
1-萘羥肟酸
英文別名
NSC 57457
Naphthohydroxamicacid
a-Naphthohydroxamic acid
1-NAPHTHOHYDROXAMIC ACID
alpha-naphthohydroxamicacid
1-NAPHTHOHYDROXAMIC ACID 98+%
HDAC Inhibitor XIX, Compound 2
1-Naphthalenecarbohydroximic acid
n-hydroxy-1-naphthalenecarboxamid
N-Hydroxy-1-naphthalenecarboxamide
所屬類(lèi)別
化學(xué)試劑:羥胺

物理化學(xué)性質(zhì)

儲(chǔ)存條件2-8°C
溶解度二甲基亞砜:≥5mg/mL
形態(tài)白色固體
顏色白色至棕褐色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H312-H302-H332
危險(xiǎn)類(lèi)別碼52
WGK Germany3
RTECS號(hào)QJ1894500
海關(guān)編碼2928009090
1-萘羥肟酸價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/08/19HY-1305381-萘羥肟酸
1-Naphthohydroxamic acid
6953-61-35mg650元
2024/08/19HY-1305381-萘羥肟酸
1-Naphthohydroxamic acid
6953-61-310mM * 1mLin DMSO720元
2024/08/19HY-1305381-萘羥肟酸
1-Naphthohydroxamic acid
6953-61-310mg1200元

常見(jiàn)問(wèn)題列表

生物活性
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(duì) HDAC8 的選擇性高于 I 類(lèi) HDAC1 和 II 類(lèi) HDAC6 (IC50 >100 μM)。1-Naphthohydroxamic acid 不會(huì)增加整體組蛋白 H4 的乙?;?,也不會(huì)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。
靶點(diǎn)

HDAC8

14 μM (IC 50 )

HDAC1

>100 μM (IC 50 )

HDAC6

>100 μM (IC 50 )

體外研究

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.
體內(nèi)研究

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.
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