DUB Inhibitor IV, b-AP15 (NSC687852, 3,5-bis((4-Nitrophenyl)methylidene)-1-prop-2-enoylpiperidin-4-one, (3E,5E)-1-Acryloyl-3,5-bis(4-nitrobenzylidene)piperidin-4-one, USP14 Inhibitor III, UCH-L5/UCH37 Inhibitor II)

Blue Ice

419, 4

Supplied as a yellow solid.

A cell-permeable bis-nitrobenzylidene-piperidinone compound that acts as a potent, reversible and selective inhibitor of 19S regulatory-particle-associated deubiquitylating enzymes (DUBs) UCH-L5 and USP-14 (IC50=2.1uM against Ub-AMC substrate), with no effect on UCH-L1, UCH-L3, USP2, USP7, USP8 and BAP1 and on the proteasomal proteolytic activities. Shown to prevent proteasomal degradation (IC50=0.8uM in MelJuSo-UbG76V-YFP cells), and cause accumulation of higher molecular weights polyubiquitinated proteins in HCT-116 cells. Preferentially induces cell-cycle arrest and apoptosis in several colon cancer and in CNS cells, and effectively suppresses tumor growth in various mouse model (5mg/kg, i.p.).

Synonyms:
USP14 Inhibitor III, UCH-L5/UCH37 Inhibitor II, NSC687852, 3, 5-bis((4-Nitrophenyl)methylidene)-1-prop-2-enoylpiperidin-4-one, (3E, 5E)-1-Acryloyl-3, 5-bis(4-nitrobenzylidene)piperidin-4-one

CAS Number:
1009817-63-4

Molecular Formula:
C₂₂H₁₇N₃O₆

Molecular Weight:
419.4

Solubility:
DMSO (100mg/ml clear, yellow solution)

Storage and Stability:
Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°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.