DBeQ

177355-84-9

C22H20N4

DMSO : >= 47 mg/mL (138.06 mM)

Autophagy; Cell Cycle/DNA Damage

DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC₅₀ value of 1.5 uM and 1.6 uM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC₅₀ of 11.5 uM. IC50 & Target: IC50: 1.5 uM (p97)^[1], 11.5 uM (Vps4)^[2] In Vitro: DBeQ is a ATP-competitive p97 inhibitor, with an IC₅₀ value of 1.5 uM and 1.6 uM for p97(wt) and p97(C522A), respectively. DBeQ inhibits p97 competitively with respect to ATP, with a K_i of 3.2 +/- 0.4 uM. DBeQ inhibits degradation of the p97-dependent substrate UbG76V-GFP, with IC₅₀ value of 2.6 uM. DBeQ (10 uM) also significantly suppresses degradation of TCRalpha-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 uM. Furthermore, DBeQ (30 uM) inhibits hyphal growth of the wild-type cell (strain YLZ0)^[2].