WP1130

Catalog #

27722-1

$180 *

Size: 5 mg

Qty

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Description

A partially-selective, cell permeable 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.

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Synonyms

Degrasyn, (S,E)–3–(6–bromopyridin–2–yl)–2–cyano–N–(1–phenylbutyl)acrylamide

Product Info

Storage and Usage

Citations

Purity

≥98% by TLC.

Format

Pale yellow powder

Formula

C19H18BrN3O

384.3 Da

Solubility

Soluble in DMSO (45 mg/ml); Ethanol (25 mg/ml)

CAS Registry #

856243-80-6

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

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