GSK481

ChemicalBook > CAS DataBase List > GSK481

Product Name: GSK481
CAS No.: 1622849-58-4
Chemical Name: GSK481
Synonyms: GSK481;CS-2186;GSK481 - GSK'481;GSK481, 10 mM in DMSO;GSK481,inhibit,Inhibitor,RIPK,GSK-481,RIP kinase,GSK 481,Receptor-interacting protein kinases;(S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)isoxazole-3-carboxamide;3-Isoxazolecarboxamide, 5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-
CBNumber: CB03122822
Molecular Formula: C21H19N3O4
Formula Weight: 377.39
MOL File: 1622849-58-4.mol

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GSK481 Property

Boiling point:: 677.0±55.0 °C(Predicted)
Density: 1.35±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: Soluble in DMSO
form: crystalline solid
pka: 11.68±0.20(Predicted)
color: Light brown to brown

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML2745
Product name: GSK′481
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $150
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML2745
Product name: GSK′481
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $593
Updated: 2024/03/01

Cayman Chemical

Product number: 20308
Product name: GSK481
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 20308
Product name: GSK481
Purity: ≥98%
Packaging: 5mg
Price: $139
Updated: 2024/03/01

Cayman Chemical

Product number: 20308
Product name: GSK481
Purity: ≥98%
Packaging: 10mg
Price: $243
Updated: 2024/03/01

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GSK481 Chemical Properties,Usage,Production

Biological Activity

gsk481 is a receptor interacting protein kinase 1 (rip1) inhibitor.the role of rip1 kinase in tumor necrosis factor mediated inflammation has resulted in its emergence as a promising target for the treatment of multiple inflammatory diseases.

in vitro

previous study showed that gsk481 could not only trigger an increase in biochemical activity but also exhibit great translation in the u937 cellular assay with ic50 of 10 nm. moreover, gsk481 also showed complete specificity for rip1 kinase against all other tested kinases when profiled over both a p33 radiolabeled assay screen. in tight-binding adp-glo ic50 evaluation with increasing atp concentration, gsk481 exhibited a shift to lower potency, which was corresponding to a competitive model. in addition, gsk481 was also found to be a potent inhibitor of s166 phosphorylation in wild-type human rip1 but was ineffective at reducing s166 phosphorylation for wild-type mouse rip1. gsk481 was also able to more potently inhibit ser166 phosphorylation in all three tested mouse rip1 mutants than in wild-type mouse [1].

target

Target	Value
RIP1

IC 50

1.3 nm for rip1

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.

GSK481 Preparation Products And Raw materials

Raw materials

Preparation Products

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1622849-58-4, GSK481Related Search:

RET Kinase inhibitor 1 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide GSK484 GSK583 GSK369796 GSK461364 GSK547 GSK-467 GSK-3326595 4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide

GSK481

CS-2186

GSK481 - GSK'481

3-Isoxazolecarboxamide, 5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-

(S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)isoxazole-3-carboxamide

GSK481,inhibit,Inhibitor,RIPK,GSK-481,RIP kinase,GSK 481,Receptor-interacting protein kinases

GSK481, 10 mM in DMSO

1622849-58-4