1244640-48-9

VU 0364739 Hydrochloride is a selective, small molecule inhibitor of phopholipase D2.

PLD2-selectivePH domain-targeting phospholipase D allosteric inhibitor with in vitro and in vivo efficacy.
VU0364739 is a PLD2-selectivePH domain-targeting phospholipase D allosteric inhibitor (PLD2/PLD1 IC50 = 100 nM/7.5 μM by enzymatic assay) th at 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 μMrespectively). VU0364739 is reported to suppress PLD2-dependent proliferation in cultures (by 56% in 48 hrs; MDA-MB-23110 μM) and alleviate the symptoms of DSS-induced colitis in mice in vivo (10 mg/kg i.p. qod).

PLD2: 20 nM (IC₅₀); PLD1: 1500 nM (IC₅₀)

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