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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;5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-3-isoxazolecarboxamide;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
$124.45
Updated
2025/07/31
Sigma-Aldrich
Product number
SML2745
Product name
GSK′481
Purity
≥98% (HPLC)
Packaging
25MG
Price
$493.05
Updated
2025/07/31
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

Uses

GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM[1].

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].

in vivo

GSK481 inhibits Ser166 phosphorylation in three mouse RIP1 mutants (IC50=18~110 nM) more potently than in wild-type mouse[1].

target

TargetValue
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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GSK481 Suppliers

China 69 United States 9 USA 1 Global 79
Musechem
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+1-800-259-7612
Fax
+1-800-259-7612
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info@musechem.com
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United States
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4660
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TargetMol Chemicals Inc.
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+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
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United States
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32435
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InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
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6391
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Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
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58
Aladdin Scientific
Tel
Email
tp@aladdinsci.com
Country
United States
ProdList
57505
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58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354;
Email
support@targetmol.com
Country
United States
ProdList
39035
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58
ApexBio Technology
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sales@apexbt.com
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United States
ProdList
6251
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Cayman Chemical Company
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cayman@caymanchem.com
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United States
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6213
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Axon Medchem LLC
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Email
info@axonmedchem.com
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United States
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763
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58

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
  • 5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-3-isoxazolecarboxamide
  • 1622849-58-4