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LifeSensors/SI9659-25mg WP-1130/SI9659-25mg WP-1130

A partially-selective DUB inhibitor that directly inhibits USP9x, USP5, USP14, and UCH37. WP1130, derived from the tyrphostin AG490, was identified in a screen for molecules that suppress IL-3 and IL-6 activation of STAT molecules. It has been subsequently shown to induce rapid accumulation of polyubiquitinated (K48/K63-linked) proteins into juxtanuclear aggresomes, block JAK2 signaling through JAK2 ubiquitination and subsequent downregulation, and exhibit antiviral activity through activation of the unfolded protein response (UPR). Typical concentration for cell culture experiments is 5 µM.



Info


FormulaC19H18BrN3O
CAS No.126288-28-7
Purity>98% (TLC), NMR (conforms)
Molecular weight384.3 Da
Physical StatePale yellow powder
SolubilityDMSO (45 mg/mL); ethanol (25 mg/mL)
StorageStore dessicated as supplied at 4oC. Store solutions at -20oC for up to 3 months
Alternate NamesDegrasyn
Chemical Name(S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide



Applications

  • Cell-based studies of USP function.
  • Benefits: cell-permeable.


Documents



References

[1] Kapuria, V. et al. Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis.  Cancer Res. 2010, 70(22):9265

[2] Batholomeusz, G.A., et al. Activation of a novel Bcr/Abl destruction pathway by WP1130 induces apoptosis of chronic myelogenous leukemia cells. Blood. 2007 109(8):3470.

[3] Kapuria, V. et al. A novel small molecule deubiquitinase inhibitor blocks Jak2 signaling through Jak2 ubiquitination. Infect. Immun. 2011, 23(12):2076.

[4] Perry, J.W., et al. Antiviral Activity of a Small Molecule Deubiquitinase Inhibitor Occurs via Induction of the Unfolded Protein Response. PLos Pathog. 2012, 8(7): Epub 2012 Jul 5.
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