proTAME 是 TAME 的一种细胞渗透性前药形式,是一种后期促进复合物/环体 (APC/C) 抑制剂。proTAME 导致细胞周期停滞在中期。
生物活性
proTAME, a cell-permeable prodrug form of TAME, is an anaphase promoting complex/cyclosome (APC/C) inhibitor. proTAME causes cell cycle arrest in metaphase.
性状
Solid
体外研究(In Vitro)
ProTAME prevents anaphase entry in mouse and bovine oocytes and also in mouse 2-cell embryos. proTAME (0-100 μM ) treatment shows dose-dependent metaphase arrest in mammalian oocytes and early cleavage embryos. And the metaphase arrest induced by this drug does not require spindle assembly checkpoint (SAC) activity.ProTAME arrest of meiosis I in mouse oocytes is due to the inhibition of APC/C. In contrast to the somatic cells, the arrest in oocytes and embryos is not reversible.proTAME (0-20 μM) dose-dependently affects morphological parameters of the spindle in oocytes and in embryos.proTAME is efficient in overcoming resistance caused by the hyperphosphorylation of CDH1 in glioblastoma cells, polo-like kinase 1 (PLK1)-based drug resistance in ovarian cancer cells and CDC20-based resistance in diffuse large B-cell lymphoma.proTAME inhibits OVCAR-3 cells gr
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Lenka Radonova, et al. ProTAME Arrest in Mammalian Oocytes and Embryos Does Not Require Spindle Assembly Checkpoint Activity. Int J Mol Sci. 2019 Sep 13;20(18):4537.[2]. Monika Raab, et al. Blocking Mitotic Exit of Ovarian Cancer Cells by Pharmaceutical Inhibition of the Anaphase-Promoting Complex Reduces Chromosomal Instability. Neoplasia. 2019 Apr;21(4):363-375.
溶解度数据
In Vitro: DMSO : 100 mg/mL (137.60 mM; Need ultrasonic)配制储备液