AdipoGen b-AP15
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Chemical. CAS 1009817-63-3. Formula C22H17N3O6. MW 419.4. b-AP15 is a specific deubiquitinase DUB inhibitor. It inhibits ubiquitin-specific-processing protease 14 USP14 and ubiquitin c-terminal hydrolase isozyme L5 UCHL5 UCH37, two 19S regulatory particle proteasome-associated DUBs. It exhibits minimal inhibition of UCHL-1, UCHL-3, USP2, USP7, USP and BAP1. Has been described to inhibit also the 20S proteasome with an IC50 comparable to that required for inhibiting the 19S regulatory particles. b-AP15 has anticancer properties and blocks tumor progression in vivo in mice and prevents organ infiltration in mouse models of myeloid leukemia. b-AP15 also renders tumor cells sensitive to TNF-mediated apoptosis by natural killer and T cells. It induces apoptosis, ER stress and autophagy in several cancer cells. b-AP15 has anti-inflammatory properties inhibiting ERK1/2 and JNK phosphorylation, increasing IkappaBalpha levels and inhibiting NF-kappaB p65.