Synonym: (S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b]-[1,4]oxazepin-3-yl)isoxazole-3-carboxamide; GSK 2882481; GSK 481; GSK-2882481; GSK-481; GSK2882481; GSK481
CAS Number: 1622849-58-4
Empirical Formula (Hill Notation): C21H19N3O4
Molecular Weight: 377.39
MDL Number: MFCD30343843
Linear Formula: C21H19N3O4
Product Type: Chemical
| assay |
≥98% (HPLC) |
| color |
white to beige |
| form |
powder |
| Quality Level |
100  |
| solubility |
DMSO: 2 mg/mL, clear |
| storage temp. |
−20°C |
| Biochem/physiol Actions: |
GSK′481 is a highly potent receptor interacting protein 1 kinase (RIP1, RIPK1) inhibitor (human/monkey RIP1 IC50 = 1.6/2.5 nM; [ATP] = 50 μM) that targets RIP1 ATP-binding pocket with high affinity (kon = 0.66/μM/sec, t1/2 = 11 min) with little potency toward non-primate RIP1 (IC50 = 2.0/3.2/6.3/7.9/>10 μM against rabbit/mouse/rat/dog/minipig RIP1) and no off-target affinity when profiled at 10 μM by a 456-kinase panel. GSK′481 blocks caspase inhibitor/TNF-induced necroptosis in human monocytic U937 cultures (IC50 = 10 nM) and inhibits S166 autophosphorylation of exogenously expressed human, but not mouse, RIP1 in HEK293T transfectants (IC50 = 2.8 nM and >10 μM, respectively). |
| WGK Germany |
WGK 3 |
| Flash Point(F) |
Not applicable |
| Flash Point(C) |
Not applicable |
| Purity |
≥98% (HPLC) |
| Storage Temp. |
−20°C |
| UNSPSC |
12352200 |
