WP-1130 | 2014

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.

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.

2014 | WP-1130 DataSheet

Alternate Name/Synonyms: (S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide; Degrasyn

Appearance: Pale yellow solid

Formulation: N/A

CAS Number: 856243-80-6

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₁₉H₁₈BrN₃O

Molecular Weight: 384.27

Cell-Permeable?: Yes

Purity: ≥98% by TLC

Solubilities: DMSO (40 mg/ml) or EtOH (25 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A selective DUB (deubiquitinases) inhibitor

MDL Number: N/A

PubChem CID: 11222830

SMILES: CCCC(C1=CC=CC=C1)NC(=O)C(=CC2=NC(=CC=C2)Br)C#N

InChi: InChI=1S/C19H18BrN3O/c1-2-7-17(14-8-4-3-5-9-14)23-19(24)15(13-21)12-16- 10-6-11-18(20)22-16/h3-6,8-12,17H,2,7H2,1H3,(H,23,24)/b15-12+/t17-/m0/s1

InChi Key: LIDOPKHSVQTSJY-VMEIHUARSA-N