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
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-
沸点
475.6±55.0 °C(Predicted)
密度
1.34±0.1 g/cm3(Predicted)
溶解度
DMSO: soluble15mg/mL, clear
酸度系数(pKa)
9.59±0.10(Predicted)
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
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.
