WP1130 (Degrasyn) --- Deubiquitinylating Enzyme (DUB) Inhibitor

Overview
Catalog #	bs-60206c-2mg-solid
Product Name	WP1130 (Degrasyn) --- Deubiquitinylating Enzyme (DUB) Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 384.27 Formula: C19 H18 Br N3 O CAS Number: 856243-80-6 InChi Key: LIDOPKHSVQTSJY-VMEIHUARSA-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 Smiles: CCC[C@H](NC(=O)/C(=C/C1C=CC=C(Br)N=1)/C#N)C1C=CC=CC=1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	WP1130 (Degrasyn) is a cell-permeable, potent and selective inhibitor of the deubiquitinylating enzymes (DUBs). At 5 μM it directly inhibits DUB activity of USP9x, USP5, USP14, UCH-L1, and UCH37, but not UCH-L3, resulting in downregulation of antiapoptotic and upregulation of proapoptotic proteins, such as MCL-1 and p53. WP1130 suppresses Bcr/Abl, JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). It did not directly suppress Jak2 kinase activity, but mediated Jak2 ubiquitination, resulting in its trafficking through HDAC6 to perinuclear aggresomes without cytokine stimulation or SOCS-1 induction.