SML2745
GSK′481
≥98% (HPLC)
Synonym(s):
(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
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About This Item
Empirical Formula (Hill Notation):
C21H19N3O4
CAS Number:
Molecular Weight:
377.39
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
N1(c2c(cccc2)OC[C@@H](C1=O)NC(=O)c3n[o]c(c3)Cc4ccccc4)C
InChI
1S/C21H19N3O4/c1-24-18-9-5-6-10-19(18)27-13-17(21(24)26)22-20(25)16-12-15(28-23-16)11-14-7-3-2-4-8-14/h2-10,12,17H,11,13H2,1H3,(H,22,25)/t17-/m0/s1
InChI key
KNOUWGGQMADIBV-KRWDZBQOSA-N
Biochem/physiol Actions
A highly selective ATP site-targeting inhibitor against human/monkey, but not non-primate, RIP1.
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).
Storage Class
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
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