1-萘羟肟酸 T13996

Product Introduction
Bioactivity


英文名: 1-Naphthohydroxamic acid

描述: 1-Naphthohydroxamic acid 是一种选择性 HDAC8抑制剂，IC50为 14 μM。它对 HDAC8的选择性高于 I 类 HDAC1 和 II 类 HDAC6，IC50大于100 μM，可诱导微管蛋白乙酰化。

体外活性: 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 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]. 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.

体内活性: 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]. 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. 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 125 mg/mL (667.77 mM)


关键字: tubulin | anti-proliferation | deacetylate | HDAC8 | Inhibitor | 1 Naphthohydroxamic acid | hyperacetylated | 1Naphthohydroxamic acid | 1-Naphthohydroxamic acid | acetylation | inhibit | clone | HDAC | Histone deacetylases

相关产品: HDAC-IN-64 | Abexinostat | (2R/S)-6-PNG | Pyroxamide | HDAC6-IN-16 | PRO-HD2 | SP-2-225 | EDO-S101 | SS-208 | UF010

相关库: Anti-Breast Cancer Compound Library | Anti-Cancer Compound Library | Microtubule-Targeted Compound Library | NF-κB Signaling Compound Library | Inhibitor Library | Epigenetics Compound Library | DNA Damage & Repair Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Chromatin Modification Compound Library

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