2-Methoxyestradiol-d 5

2-Methoxyestradiol -d 5 (2-ME2-d 5; NSC-659853-d 5 ) is the deuterated-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2; NSC-659853) is an endogenous steroid metabolite generated from 17β-estradiol, possessing various activities such as antitumor and antiangiogenic effects. 2-Methoxyestradiol competitively binds to the colchicine-binding site of tubulin ( tubulin ), interfering with microtubule assembly dynamics. 2-Methoxyestradiol inhibits CYP1A1/CYP1B1, HIF-1α/2α, and superoxide dismutase, activates the JNK signaling pathway, elevates ROS levels, and induces cell cycle arrest and apoptosis ( apoptosis ). 2-Methoxyestradiol is used in cancer-related research, such as breast cancer, prostate cancer, and multiple myeloma ^{[1] [2] [3] [4]}.

References:
[1]. Lakhani NJ, et al. 2-Methoxyestradiol, a promising anticancer agent. Pharmacotherapy. 2003 Feb;23(2):165-72.
[2]. Mooberry SL, et al. Mechanism of action of 2-methoxyestradiol: new developments. Drug resistance updates: reviews and commentaries in antimicrobial and anticancer chemotherapy. 2003 Dec;6(6):355-61.
[3]. LaVallee TM, et al. 2-Methoxyestradiol inhibits proliferation and induces apoptosis independently of estrogen receptors alpha and beta. Cancer research. 2002 Jul 01;62(13):3691-7.
[4]. Pribluda VS, et al. 2-Methoxyestradiol: an endogenous antiangiogenic and antiproliferative drug candidate. Cancer metastasis reviews. 2000;19(1-2):173-9.