UPS Inhibitor

SI9669: b-AP15

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Specifications

Blocks 26S proteasome activity by inhibiting the ubiquitin C-terminal hydrolase 5 (UCHL5) and ubiquitin-specific peptidase 14 (USP14) activities of the 19S regulatory subunit without affecting the catalytic activity of the 20S core subunit. b-AP15 displays several differences to bortezomib including insensitivity to over-expression of the anti-apoptotic mediator Bcl-2 and anti-tumor activity in four solid tumor models.

Info

Purity >98% (TLC), NMR (conforms)
Quantity 5 mg, 25 mg
Molecular Weight 419.4 Da
Physical State Pale yellow powder
Solubility DMSO (35 mg/mL)
CAS No. 1009817-63-3
Storage 4°C, (-20°C Long term). The product can be shipped at room temperature.

Additional information

Weight

5 mg, 25 mg

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Applications

  • Validation studies of the deubiquitinating activities of the 19S regulatory particle as a drug target
  • Cell-based and in vitro characterization of UCH-L5 or USP14 activity
  • Inhibition of the 26S proteasome through a mechanism distinct from inhibition of 20S catalytic activity

Benefits

  • D’Arcy P.  et al. Inhibition of proteasome deubiquitinating activity as a new cancer therapy. Nature Medicine 2011 17:1636
  • D’Arcy P. and Linder S. Proteasome deubiquitinases as novel targets for cancer therapy. Int. J. Biochem. Cell Biol. 2012 E Published ahead of print.

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