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863774-58-7

中文名稱 2,3,4,6,7,8-六氫-4-(3-羥基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮
英文名稱 Dimethylenastron
CAS 863774-58-7
分子式 C16H18N2O2S
分子量 302.39
MOL 文件 863774-58-7.mol
更新日期 2024/11/05 13:11:13
863774-58-7 結(jié)構(gòu)式 863774-58-7 結(jié)構(gòu)式

基本信息

中文別名
化合物DIMETHYLENASTRON
EG5抑制劑(DIMETHYLENASTRON)
2,3,4,6,7,8-六氫-4-(3-羥基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮
英文別名
enastron
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-
所屬類別
生物化工:激動劑抑制劑

物理化學性質(zhì)

沸點475.6±55.0 °C(Predicted)
密度1.34±0.1 g/cm3(Predicted)
儲存條件2-8°C
溶解度DMSO:可溶15mg/mL,澄清
酸度系數(shù)(pKa)9.59±0.10(Predicted)
形態(tài)粉末
顏色白色至米色

安全數(shù)據(jù)

常見問題列表

生物活性
Dimethylenastron 是一種有效的、特異性的、可逆的 kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) 抑制劑,其IC50值為200 nM。Dimethylenastron 可誘導人多發(fā)性骨髓瘤細胞的有絲分裂停滯和凋亡并上調(diào) Hsp70 的表達。
靶點
TargetValue
KSP
(Cell-free assay)
200 nM
體外研究

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.

體內(nèi)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.

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