VU0359595 is a potent and selective inhibitor of PLD1. Phospholipase D (PLD) isozymes mediate phospholipid hydrolysis and transphosphatidylation. Until now, two mammalian isoforms of PLD, PLD1, and PLD2, have been identified. It has been identified that PLD has been implicated in a human cancer cell progression, actin cytoskeleton reorganization and cell motility . In vitro: VU0359595 was an inhibitor of PLD1 with an IC50 of 3.7 nM. VU0359595 showed >1,700-fold selectivity over PLD2. The IC50 of was VU0359595 against PLD2 was 6.4 μM . Preliminary evidence has demonstrated that VU0359595 showed no interaction with the catalytic site of PLD, but may bind and inhibit PLD through an allosteric site . At 500 nM, VU0359595 significantly reduced the PLD activity in astroglial cultures from wild-type mice by 58% . In cells stimulated by 1% FCS, VU0359595 decreased cell proliferation in wild-type and PLD2-deficient cells at a concentration of 500 nM . VU0359595 (500 nM) significantly reduced cell growth in cells stimulated by either mitogen .

Product information

CAS Number: 1246303-14-9

Molecular Weight: 497.43

Formula: C25H29BrN4O2

Chemical Name: (1R,2R)-N-[(2S)-1-[4-(5-bromo-2-oxo-2,3-dihydro-1H-1,3-benzodiazol-1-yl)piperidin-1-yl]propan-2-yl]-2-phenylcyclopropane-1-carboxamide

Smiles: C[C@@H](CN1CCC(CC1)N1C2C=CC(Br)=CC=2NC1=O)NC(=O)[C@@H]1C[C@H]1C1C=CC=CC=1

InChiKey: JSVNNLRZCJAYTQ-ORYQWCPZSA-N

InChi: InChI=1S/C25H29BrN4O2/c1-16(27-24(31)21-14-20(21)17-5-3-2-4-6-17)15-29-11-9-19(10-12-29)30-23-8-7-18(26)13-22(23)28-25(30)32/h2-8,13,16,19-21H,9-12,14-15H2,1H3,(H,27,31)(H,28,32)/t16-,20-,21+/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

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