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Biochem/physiol Actions
PLD2-selective, PH domain-targeting phospholipase D allosteric inhibitor with in vitro and in vivo efficacy.
VU0364739 is a PLD2-selective, PH domain-targeting phospholipase D allosteric inhibitor (PLD2/PLD1 IC50 = 100 nM/7.5 μM by enzymatic assay) that selectively suppresses the cellular PLD activity in GFP-PLD2-overexpressing HEK293 cells over PMA-stimulated non-small-cell lung cancer (NSCLC) Calu-1 cells with predominant PLD1 activity (IC50 = 20 nM and 1.5 μM, respectively). VU0364739 is reported to suppress PLD2-dependent proliferation in cultures (by 56% in 48 hrs; MDA-MB-231, 10 μM) and alleviate the symptoms of DSS-induced colitis in mice in vivo (10 mg/kg i.p. qod).
Disclaimer
Hygroscopic
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
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