863774-58-7
863774-58-7 结构式
基本信息
EG5抑制剂(DIMETHYLENASTRON)
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
Eg5 Inhibitor III
Eg5 Inhibitor III(Dimethylenastron)
Dimethylenastron - Eg5 inhibitor III
Eg5 Inhibitor III, Dimethylenastron - CAS 863774-58-7 - Calbiochem
2,3,4,6,7,8-Hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-5(1H)-quinazolinone
4-(3-Hydroxyphenyl)-7,7-dimethyl-2-thioxo-2,3,4,6,7,8-hexahydroquinazolin-5(1H)-one
5(1H)-Quinazolinone, 2,3,4,6,7,8-hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-
物理化学性质
常见问题列表
| Target | Value |
|
KSP
(Cell-free assay) | 200 nM |
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.
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.