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。

1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC 50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC 50 >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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HDAC8 14 μM (IC50) HDAC1 >100 μM (IC

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 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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[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.
[2]. Oehme I, et al. Histone deacetylase 8 in neuroblastoma tumorigenesis. Clin Cancer Res. 2009 Jan 1;15(1):91-9.

In Vitro: DMSO : 125 mg/mL (667.77 mM; Need ultrasonic)配制储备液