proTAME

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

proTAME 是 TAME 的细胞渗透性前药，TAME 是一种后期促进复合物/环体 (APC/C) 抑制剂，与 APC 结合优先抑制 APC/C(Cdc20)。

proTAME is a cell permeable prodrug of TAME, which is an anaphase-promoting complex/cyclosome (APC/C) inhibitor that binds to the APC preferentially suppresses APC/C(Cdc20); arrests cells in metaphase without perturbing the spindle, but is dependent on the spindle assembly checkpoint (SAC); efficiently targets osteosarcoma in vitro combined with chemotherapeutic agents.

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 growth with an IC50 of 12.5 μM.

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pro-Tosyl-L-Arginine Methyl Ester

Proteasome/Ubiquitin

E3 Ubiquitin Ligase

E3 Ubiquitin Ligase

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1362911-19-0

726.8

C34H38N4O12S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (137.60 mM)

O=C(OCOC(/N=C(NCCC[C@H](NS(C1=CC=C(C)C=C1)(=O)=O)C(OC)=O)/NC(OCOC(CC2=CC=CC=C2)=O)=O)=O)CC3=CC=CC=C3

10,12-Dioxa-6,8-diazatetradec-6-enoic acid, 2-[[(4-methylphenyl)sulfonyl]amino]-9,13-dioxo-14-phenyl-7-[[[[(2-phenylacetyl)oxy]methoxy]carbonyl]amino]-, methyl ester, (2S)-

(-20℃)

With Ice Pack

≥ 2 years