Cell-permeable. WP1130 acts as a partly selective DUB (deubiquitinases) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37, which are known to regulate survival protein stability and 26S proteasome function. WP1130-mediated inhibition of tumor-activated DUBs results in downregulation of antiapoptotic and upregulation of proapoptotic proteins, such as MCL-1 and p53. Blocks JAK2 signaling via JAK2 ubiquitination.
Sequence:
(S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide
Molecular Weight:
~384.27
Solubility:
DMSO (~40mg/ml) or EtOH (~25mg/ml)
Storage and Stability:
Lyophilized powder may be stored at -20 degrees C. Stable for 12 months at -20 degrees C. Reconstitute with DMSO. Aliquot to avoid repeated freezing and thawing. Store at -20 degrees C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
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