bs-60206C
[Life Science]
WP1130 (Degrasyn) --- Deubiquitinylating Enzyme (DUB) Inhibitor
DATASHEET
Formulation Powder
Storage: Store in dry, dark place at -20C for 1 year.
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
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.
Size: 10mg solid,2mg solid 10mg solid,2mg solid
Applications: Life Science()
For research use only. Not intended for diagnostic or therapeutic use.