VU0155072

Biochem/physiol Actions

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.

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Code Description Colour Quality Level Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576719 VU0155072 white to beige 100 SIGMA-ALDRICH 2-8°C
£852.43 (exc VAT) per EACH
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3576720 VU0155072 white to beige 100 SIGMA-ALDRICH 2-8°C
£218.68 (exc VAT) per EACH
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