2,3,4,6,7,8-六氢-4-(3-羟基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮
生物活性靶点体外研究体内研究 用途与合成方法 MSDS 2,3,4,6,7,8-六氢-4-(3-羟基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮价格(试剂级) 上下游产品信息
| 中文名称 | 2,3,4,6,7,8-六氢-4-(3-羟基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮 |
|---|---|
| 中文同义词 | 2,3,4,6,7,8-六氢-4-(3-羟基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮;EG5抑制剂(DIMETHYLENASTRON);化合物DIMETHYLENASTRON;DIMETHYLENASTRON,抑制剂 |
| 英文名称 | Dimethylenastron |
| 英文同义词 | Dimethylenastron;2,3,4,6,7,8-Hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-5(1H)-quinazolinone;Eg5 Inhibitor III(Dimethylenastron);Eg5 Inhibitor III, Dimethylenastron - CAS 863774-58-7 - Calbiochem;Dimethylenastron - Eg5 inhibitor III;Eg5 Inhibitor III;enastron;5(1H)-Quinazolinone, 2,3,4,6,7,8-hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo- |
| CAS号 | 863774-58-7 |
| 分子式 | C16H18N2O2S |
| 分子量 | 302.39 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂;标准品 |
| Mol文件 | 863774-58-7.mol |
| 结构式 | ![]() |
2,3,4,6,7,8-六氢-4-(3-羟基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮 性质
| 沸点 | 475.6±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.34±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | DMSO:可溶15mg/mL,澄清 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 9.59±0.10(Predicted) |
| 颜色 | 白色至米色 |
2,3,4,6,7,8-六氢-4-(3-羟基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮 用途与合成方法
生物活性
Dimethylenastron 是一种有效的、特异性的、可逆的 kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) 抑制剂,其IC50值为200 nM。Dimethylenastron 可诱导人多发性骨髓瘤细胞的有丝分裂停滞和凋亡并上调 Hsp70 的表达。
靶点
| Target | Value |
| KSP (Cell-free assay) | 200 nM |
体外研究
Dimethylenastron is a potent Eg5 inhibitor, with an IC 50 of 200 nM. Dimethylenastron exhibits no inhibition of five other kinesin subfamilies (kinesin 1/4/7/10 and one ungrouped-originating from 4 different organisms). Dimethylenastron (0.5, 1 μM) causes accumulation of cells in G2/M in HeLa cells. Dimethylenastron (3 and 10 μM) concentration-dependently suppresses the migratory ability of the cancer cells in PANC1 pancreatic cancer cells after treatment for 24 h, but does not inhibit the proliferation of cancer cells at 24 h until 72 h. Dimethylenastron also reduces invasion ability of the cancer cells.
体内研究
Dimethylenastron (1.0 µmol) induces a milder scarring but the length of bleb survival is not significantly prolonged compared with the control group. Dimethylenastron (1.0 µmol) reveals a markedly reduced ratio of intraocular pressure and a milder, but not obviously reduced, subconjunctival fibrotic reaction in the rabbits treated with glaucoma filtration surgery.
安全信息
| WGK Germany | 3 |
|---|
MSDS信息
2,3,4,6,7,8-六氢-4-(3-羟基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-19944 | Dimethylenastron | 1 mg | 320元 | |
| 2024/08/19 | HY-19944 | 2,3,4,6,7,8-六氢-4-(3-羟基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮 Dimethylenastron | 863774-58-7 | 5mg | 700元 |



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