Dimethylenastron

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

有丝分裂驱动蛋白 Eg5 的小分子抑制剂；体外抑制内皮细胞增殖和迁移。

A small molecule inhibitor of the mitotic kinesin Eg5; inhibits endothelial cell proliferation and migration in vitro; exhibits a shorter mitotic arrest, bipolar or multipolar karyokinesis, followed by apoptosis of the daughter cells in dimethylenastron-treated tetraploid cells.

Dimethylenastron is a potent Eg5 inhibitor, with an IC50 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.

Dimethylenastron

Cytoskeleton/Cell Adhesion Molecules

Kinesin

Eg5

Cancer

——

863774-58-7

302.3913

C16H18N2O2S

>98% (HPLC)

DMSO: ≥ 31 mg/mL

O=C1C2=C(NC(NC2C3=CC=CC(O)=C3)=S)CC(C)(C)C1

5(1H)-Quinazolinone, 2,3,4,6,7,8-hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-

(-20℃)

With Ice Pack

≥ 2 years