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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
6953-61-3
- 规格：
1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 1 mg | 产品价格： | ￥175.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥404.0 |
| 规格： | 10 mg | 产品价格： | ￥665.0 |
| 规格： | 25 mg | 产品价格： | ￥1396.0 |
| 规格： | 50 mg | 产品价格： | ￥2235.0 |
| 规格： | 100 mg | 产品价格： | ￥3580.0 |
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1-Naphthohydroxamic acid
CAS No. : 6953-61-3
MCE 国际站：1-Naphthohydroxamic acid
产品活性：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。
研究领域：Cell Cycle/DNA Damage | Epigenetics
作用靶点：HDAC
In Vitro: 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.
In Vivo: 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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文献和实验% SDS 890mL dH2 O Maleic Acid Buffer (1L) 11.61g Maleic Acid 8.766g NaCl Fill with dH2 O *check pH 7.5 with NaOH pellets (~7g) *Autoclave* Diluting Ab 1:10,000 (30mL) 3mL Blocking Buffer stock
Detection of ras Gene Mutations Using Oligonucleotide Ligation Technology
acquire oncogenic potential primarily as a result of point, missense mutations in codons 12, 13, or 61, producing single amino-acid substitutions that alter the ability of the protein to bind or hydrolyze GTP. The net consequence of somatic ras missense
The GTPase Cycle How Dominant Inhibitory Mutants Block the Biological Functions of Small GTPases
of the normal regulatory mechanisms. This technique has been used very successfully with many small GTPases and is based largely on the early work on “natural” Ras mutants (associated with cancers), which were found to contain amino-acid substitutions
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