GSK'481

Names

[ Name ]:
GSK'481

[Synonym ]:
3-Isoxazolecarboxamide, 5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-
5-Benzyl-N-[(3S)-5-methyl-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepin-3-yl]-1,2-oxazole-3-carboxamide
GSK481a
GSK-481
(S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)isoxazole-3-carboxamide
GSK'481

Biological Activity

[Description]:

GSK'481 can inhibit RIP1 WT S166 phosphorylation in human vs mouse plasmids overexpressed in HEK293T cellsGSK'481 have approximately equivalent RIP1 FP potencies against human andcynomolgus monkey RIP1 but was >100-fold less potent against nonprimate RIP1

[Related Catalog]:

Signaling Pathways >> Apoptosis >> RIP kinase

Research Areas >> Cancer

[References]

[1]. Harris PA et al. DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors. J Med Chem, 2016 Mar 10, 59(5):2163-78.

[Related Small Molecules]

Necrostatin-1 | GSK872 | GSK2982772 | WEHI-345 | RIPA-56 | GSK 583 | RIP2 kinase inhibitor 1 | RIP2 kinase inhibitor 2 | Nec-4

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
677.0±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₁H₁₉N₃O₄

[ Molecular Weight ]:
377.393

[ Flash Point ]:
363.2±31.5 °C

[ Exact Mass ]:
377.137543

[ PSA ]:
84.67000

[ LogP ]:
2.06

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.653

[ Storage condition ]:
-20℃