WP1130 Chemical Properties

Density 

1.358

storage temp. 

-20°

solubility 

Soluble in DMSO (up to 45 mg/ml), or in Ethanol (up to 25 mg/ml).

form 

solid

color 

Yellow

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

WP1130 Usage And Synthesis

Description

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.

Uses

(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide can be used in biological study of drug screening and proteomic and metabolomic profiling to identify drug action mechanisms of breast cancer impaired pathogenicity.

target

DUB

References

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

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