Catalog Number: 5330
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 Activity
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:
    >98%
  • Storage:
    Store at -20°C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. cIAP1 and cIAP2 facilitate cancer cell survival by functioning as E3 ligases that promote RIP1 ubiquitination.
    Bertrand et al.
    Mol. Cell, 2008;30:689
  2. Smac mimetics and innate immune stimuli synergize to promote tumor death.
    Beug et al.
    Nat.Biotechnol., 2014;32:182
  3. Cytoprotective effects of IAPs revealed by a small molecule antagonist.
    Galbán et al.
    Biochem.J., 2009;417:765

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