Revision 1

#56003Store at -20C

1 mg

Cell Signaling Technology

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Support: 877-678-TECH (8324)

Web: [email protected] cellsignal.com

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For Research Use Only. Not for Use in Diagnostic Procedures.

Background

SM-164 is a bivalent, cell-permeable, non-peptide, SMAC mimetic and potent XIAP inhibitor with an IC50 value of 1.39 nM. SM-164 binds to the BIR2 and BIR3 domains of XIAP and effectively inhibits cell growth and induces apoptosis in HL-60 leukemia cells (1). It also activates caspase-3 and caspase-9 that, in turn, induce apoptosis in leukemia cells (1,2). In breast cancer mouse xenograft models, SM-164 in combination with TNF-related apoptosis-inducing ligand (TRAIL) has been shown to reduce tumor volume by 80%. SM-164 is an effective apoptotic inducer of tumor cells and tissues and is a promising candidate for a new class of anticancer drugs (2). Treatment of RIP3-positive cells with SM-164 in combination with TNF-alpha and the caspase inhibitor Z-VAD, leads to necroptosis (3).

  1. Sun, H. et al. (2007) J Am Chem Soc 129, 15279-94.
  2. Lu, J. et al. (2008) Cancer Res 68, 9384-93.
  3. Sun, L. et al. (2012) Cell 148, 213-27.

Molecular Formula

C62H84N14O6

Molecular Weight

1121.4 g/mol

Purity

>98%

CAS

957135-43-2

Solubility

Soluble in DMSO at 50 mg/mL.

Storage

Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Directions for Use

SM-164 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 5 mg of powder in 446 μL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

Background References

    Cross-Reactivity Key

    H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected

    Trademarks and Patents

    Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
    All other trademarks are the property of their respective owners. Visit cellsignal.com/trademarks for more information.

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