2-Naphthalenecarboxamide, N-[(1S)-2-[4-(5-chloro-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]-1-methylethyl]-, hydrochloride (1:1)

2-Naphthalenecarboxamide, N-[(1S)-2-[4-(5-chloro-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]-1-methylethyl]-, hydrochloride (1:1) Property

solubility 

Soluble to 100 mM in DMSO and to 50 mM in ethanol

Hazard and Precautionary Statements (GHS)

2-Naphthalenecarboxamide, N-[(1S)-2-[4-(5-chloro-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]-1-methylethyl]-, hydrochloride (1:1) Chemical Properties,Usage,Production

Uses

VU0155069 hydrochloride (CAY10593 hydrochloride) is a potent selective phospholipase D (PLD) inhibitor. The IC50 values for PLD1 and PLD2 are 46 and 933 nM, respectively. VU0155069 hydrochloride inhibits migration of human and mouse breast cancer cell lines[1][2].

Biological Activity

VU 0155069 is a potent and selective phospholipase D1 (PLD1) inhibitor (IC50 values are 46 and 933 nM for PLD1 and PLD2 respectively). Inhibits migration of human and mouse breast cancer cell lines in transwell assays.

IC 50

PLD1: 46 nM (IC₅₀)

storage

Store at -20°C

References

[1] Scott SA, et al. Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nat Chem Biol. 2009 Feb;5(2):108-17. DOI:10.1038/nchembio.140
[2] Lewis JA,et al. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1916-20. DOI:10.1016/j.bmcl.2009.02.057
[3] Barclay Z, et al. Attenuated PLD1 association and signalling at the H452Y polymorphic form of the 5-HT(2A) receptor. Cell Signal. 2013 Apr;25(4):814-21. DOI:10.1016/j.cellsig.2013.01.004