AEG 40730 dihydrochloride
Chemical Name: 222,Trifluoro-N-[[(2S)-1-(N-methyl-L-analyl-L-threonyl)-2-pyrrolidinyl]methyl]-N-(2-phenylethyl)acetamide, diethyl ether with 2,4-hexadiyne-1.6-diol dihydrochloride
Biological ActivityIAP antagonist; binds to the BIR3 domain of cIAP1, cIAP2 and XIAP with nanomolar affinity. Reduces cIAP1, cIAP2 and XIAP protein levels in human breast cancer MDA-MB-231 cells. Induces apoptosis in combination with TNF, and potentiates TRAIL-mediated apoptosis in human colorectal carcinoma HCT 116 cells. Cell permeable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Smac mimetics and innate immune stimuli synergize to promote tumor death.
Beug S, Tang V, Lacasse E, Cheung H, Beauregard C, Brun J, Nuyens J, Earl N, St-Jean M, Holbrook J, Dastidar H, Mahoney D, Ilkow C, Le Boeuf F, Bell J, Korneluk R
Nat Biotechnol, 2014;32(2):182-90.
Cytoprotective effects of IAPs revealed by a small molecule antagonist.
Galbán et al.
cIAP1 and cIAP2 facilitate cancer cell survival by functioning as E3 ligases that promote RIP1 ubiquitination.
Bertrand et al.
Mol. Cell, 2008;30:689
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