VPS4 inhibitor 4-107 is a DBeQ derivative and vacuolar protein sorting 4 (VPS4) AAA-ATPase inhibitor (IC50=3.7 uM, VPS4B), inhibits VPS4 ATPase activity, induces CASP8-mediated apoptosis.
VPS4 inhibitor 4-107 is modestly selective for VPS4B in vitro over VCP (IC50=8.6 uM).
VPS4 inhibitor 4-107 4-107 (1 μM) does not induce ER stress or the accumulation of polyubiquitinated proteins, unlike CB-5083.
VPS4 inhibitor 4-107 exhibits improved cellular potency and selectivity for VPS4 compared with DBeQ.
4-107 induces ESCRT accumulation on LC3-positive autophagosomal membranes.
4-107 exhibits lysosomotropic properties and disrupts endolysosomal membrane integrity.
4-107 induces CASP8-mediated VPS4-sensitive cell death
4-107 (5 mg/kg/day, i.p.) suppresses tumor growth in syngeneic mouse model of neuroblastoma, without causing severe toxicity in mice.
Physicochemical Properties
M.Wt
370.46
Formula
C23H22N4O
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
N2,N4-dibenzyl-8-methoxyquinazoline-2,4-diamine
References
1. Fundora KA, et al. J Pharmacol Exp Ther. 2025 Feb 28;392(4):103524.
