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SML3886

Sigma-Aldrich

VU0364739 hydrochloride

≥98% (HPLC)

Synonym(s):

JWJ, ML271, N-(2-(1-(3-Fluorophenyl)-4-oxo-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)-2-naphthamide hydrochloride, N-[2-[1-(3-Fluorophenyl)-4-oxo-1,3,8-triazaspiro[4.5]dec-8-yl]ethyl]-2-naphthalenecarboxamide hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C26H27FN4O2·HCl
CAS Number:
Molecular Weight:
482.98
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

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).

Caution

Hygroscopic

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Comparison of two procedures for tracing participants in an epidemiologic cohort study
Epidemiology (Cambridge, Mass.), 1(2), 157-160 (1990)
Kinetic disruption of lipid rafts is a mechanosensor for phospholipase D
Nature Communications, 7, 13873-13873 (2016)
Chaithanya Chelakkot et al.
Scientific reports, 7(1), 1573-1573 (2017-05-10)
Ulcerative colitis is a multi-factorial disease involving a dysregulated immune response. Disruptions to the intestinal epithelial barrier and translocation of bacteria, resulting in inflammation, are common in colitis. The mechanisms underlying epithelial barrier dysfunction or regulation of tight junction proteins

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