Nexinhib 20

Names

[ Name ]:
Nexinhib 20

[Synonym ]:
(1Z)-4,4-dimethyl-1-(3-nitrophenyl)-2-(1H-1,2,4-triazol-1-yl)pent-1-en-3-one
4,4-Dimethyl-1-(3-nitro-phenyl)-2-[1,2,4]triazol-1-yl-pent-1-en-3-one
(1Z)-4,4-Dimethyl-1-(3-nitrophenyl)-2-(1H-1,2,4-triazol-1-yl)-1-penten-3-one
MFCD00219515
1-Penten-3-one, 4,4-dimethyl-1-(3-nitrophenyl)-2-(1H-1,2,4-triazol-1-yl)-, (1Z)-
4,4-dimethyl-1-(3-nitrophenyl)-2-(1H-1,2,4-triazol-1-yl)pent-1-en-3-one
(Z)-4,4-Dimethyl-1-(3-nitro-phenyl)-2-[1,2,4]triazol-1-yl-pent-1-en-3-one

Biological Activity

[Description]:

Nexinhib 20 is a novel small molecule neutrophil exocytosis inhibitor (IC50=0.33 uM) that specifically inhibits Rab27a-JFC1 binding (IC50=2.6 uM) but does not interfere with the interaction of other Rab GTPases and effectors; does not induce apoptosis or cell death, regulates exocytosis-dependent neutrophil functions and inhibits MPO secretion from human neutrophils; also reversiblely and potently inhibits extracellular production of superoxide anion and the up-regulation of activation signature molecules, including CD11b and CD66b; significantly decreased tissue infiltration by inflammatory neutrophils in vivo.

[References]

References 1. Johnson JL, et al. J Biol Chem. 2016 Dec 9;291(50):25965-25982. View Related Products by Target Small GTPase

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
508.2±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₅H₁₆N₄O₃

[ Molecular Weight ]:
300.313

[ Flash Point ]:
261.2±32.9 °C

[ Exact Mass ]:
300.122253

[ LogP ]:
2.50

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.601

Related Compounds

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