856243-80-6

WP1130 (856243-80-6) is a novel DUB inhibitor directly inhibiting USP9x, USP5, USP14 and UCH37 inducing rapid accumulation of polyubiquitinated proteins. Triggers tumor cell apoptosis.1 Blocks Jak2 signaling via Jak2 ubiquitination.2 WP-1130 causes ablation of the oncogenic transcription factor ERG in prostate cancer cells.3 See methyl analog WP1066.

DUB

1) Kapuria et al. (2010), Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis; Cancer Res., 70 9265 2) Kapuria et al. (2011), A novel small molecule deubiquitinase inhibitor blocks Jak2 signaling through Jak2 ubiquitination; Cell Signal., 23 2076 3) Wang et al. (2014), Ablation of the oncogenic transcription factor ERG by deubiquitinase inhibition in prostate cancer; Proc. Natl. Acad. Sci. USA, 111 4251