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
- CAS号:863774-58-7
- 英文名:Dimethylenastron
- 中文名: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
- CBNumber:CB41115853
- 分子式:C16H18N2O2S
- 分子量:302.39
- MOL File:863774-58-7.mol
- 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: soluble15mg/mL, clear
- 酸度系数(pKa) :9.59±0.10(Predicted)
- 形态 :powder
- 颜色 :white to beige
- WGK Germany :3
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、用途与生产工艺
- 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。
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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.
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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.
- 更新日期:2024/11/08
- 产品编号:HY-19944
- 产品名称:Dimethylenastron
- CAS编号:
- 包装:1 mg
- 价格:320元
- 更新日期:2024/11/08
- 产品编号:HY-19944
- 产品名称: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 Dimethylenastron
- CAS编号:863774-58-7
- 包装:5mg
- 价格:700元
- 公司名称:TOCRIS-US
- 联系电话:--
- 电子邮件:customerservice@tocris.co.uk
- 国家:英国
- 产品数:5726
- 优势度:77
- 公司名称:Fluorochem Ltd
- 联系电话:--
- 电子邮件:vernam@fluorochem.co.uk
- 国家:英国
- 产品数:6375
- 优势度:65