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AEG 40730 dihydrochloride

Catalog #: 5330 Datasheet / COA / SDS

Discontinued Product

5330 has been discontinued.
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AEG 40730 dihydrochloride | CAS No. 1883545-50-3 | IAP Inhibitors
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Description: IAP antagonist; induces apoptosis

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

Purity: ≥97%

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Biological Activity

AEG 40730 dihydrochloride is an IAP 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.

Technical Data

M.Wt:
1120.06
Formula:
C52H68F6N8O8.2HCl
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
≥97%
Storage:
Store at -20°C
CAS No:
1883545-50-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. 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.
  2. Cytoprotective effects of IAPs revealed by a small molecule antagonist.
    Galbán et al.
    Biochem.J., 2009;417:765
  3. 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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