PLD2-selective, PH domain-targeting phospholipase D allosteric inhibitor with in vitro and in vivo efficacy.
VU0155072 is a PLD2-selective, PH domain-targeting allosteric phospholipase D inhibitor (human PLD2/PLD1 IC50 = 140 nM/5.1 μM vs. PH/PX-deleted rat PLD1 IC50 >20 μM; cellular PLD IC50 = 110 nM/GFP-PLD2-overexpressing HEK293 vs. 1 μM/PMA-stimulated Calu-1 with predominant PLD1 activity) that selectively suppresses PLD2-dependent MDA-MB-231 invasion in cultures (by 60% in 48 hrs; 200 nM) and exhibits in vivo efficacy in murine models of DSS-induced colitis (4 mg/kg/day p.o.) and breast tumor-associated macrophages/neutrophils infiltration (75 μg/0.11 μL/kg/hr via osmotic pump). Use low concentrations (<5 μM) for cell treatment to avoid dual PLD1/2 inhibition.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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