1-萘羟肟酸
1-NAPHTHOHYDROXAMIC ACID
| 货号 | 包装规格 | 纯度/级别 | 交货周期 | 价格 | 数量 |
|---|---|---|---|---|---|
| YB562690-250mg | 250mg | 98% | 现货 | ||
| YB562690-500mg | 500mg | 98% | 现货 | ||
| YB562690-1g | 1g | 98% | 现货 |
| 中文名称 | 1-萘羟肟酸 |
|---|---|
| 英文名称 | 1-NAPHTHOHYDROXAMIC ACID |
| 别名 | 1-萘羟肟酸 |
| Cas No. | 6953-61-3 |
| MDL No. | MFCD00059546 |
| 精确分子量 | 187.06333 |
| Smiles | C1C=C2C=CC=C(C(NO)=O)C2=CC=1 |
| 密度 | 1.291±0.06 g/cm3(Predicted) |
|---|---|
| 信号词 | 警告 |
| 危险类别(旧) | 52 |
| 熔点 | 176-178 °C |
| 海关编码 | 2928009090 |
| 特性 | * |
| 水溶解性 | 二甲基亚砜：≥5mg/mL |
| 符号 | GHS07 |
| 存储要求 | 室温储存 |
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。
靶点
|
HDAC8 14 μM (IC 50 ) |
HDAC1 >100 μM (IC 50 ) |
HDAC6 >100 μM (IC 50 ) |
体外研究
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. |
体内研究
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. |
