tcsc2717 DBeQ

DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC₅₀ value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC₅₀ of 11.5 μM.

IC50 & Target: IC50: 1.5 μM (p97)^[1], 11.5 μM (Vps4)^[2]

In Vitro: DBeQ is a ATP-competitive p97 inhibitor, with an IC₅₀ value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively. DBeQ inhibits p97 competitively with respect to ATP, with a K_i of 3.2 ± 0.4 μM. DBeQ inhibits degradation of the p97-dependent substrate UbG76V-GFP, with IC₅₀ value of 2.6 μM. DBeQ (10 μM) also significantly suppresses degradation of TCRα-GFP, induces CHOP but does not increase p21 level. Moreover, DBeQ inhibits the viability of MRC-5, Hek293, HeLa and RPMI8226 cells, with GI₅₀s of 6.6 ± 2.9, 4 ± 0.6, 3.1 ± 0.5 and 1.2 ± 0.3, respectively^[1]. DBeQ potently inhibits the AAA ATPase p97 by specifically binding to the ATPase site of its D2 domain (p97D2). DBeQ also inhibits Vps4, with an IC₅₀ of 11.5 μM. Furthermore, DBeQ (30 μM) inhibits hyphal growth of the wild-type cell (strain YLZ0)^[2].