SML3886
VU0364739 hydrochloride
≥98% (HPLC)
别名:
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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所有图片(2)
About This Item
经验公式（希尔记法）:
C26H27FN4O2·HCl
CAS号:
分子量:
482.98
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77
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生化/生理作用
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).
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).
注意
Hygroscopic
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
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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