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GSK-481
CAS No. 1622849-58-4
GSK-481( GSK481 | GSK'481 )
Catalog No. M12392 CAS No. 1622849-58-4
A highly potent, monokinase selective and ATP-competitive inhibitor of RIP1 kinase with biochemical IC50 of 10 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 45 | In Stock |
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| 2MG | 29 | In Stock |
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| 5MG | 41 | In Stock |
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| 10MG | 67 | In Stock |
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| 25MG | 124 | In Stock |
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| 50MG | 200 | In Stock |
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| 100MG | 323 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameGSK-481
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NoteResearch use only, not for human use.
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Brief DescriptionA highly potent, monokinase selective and ATP-competitive inhibitor of RIP1 kinase with biochemical IC50 of 10 nM.
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DescriptionA highly potent, monokinase selective and ATP-competitive inhibitor of RIP1 kinase with biochemical IC50 of 10 nM; displays complete specificity for RIP1 kinase over a panel of 456 kinases; exhibits excellent translation in the U937 cellular assay with IC50 of 10 nM, demonstrates significant blockage of the induced RIP1 autophosphorylation at Ser166 in HT29 cells; possesses good pharmacokinetic profiles in rodents.
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In VitroGSK481 (300 nM; 2 hours; Jurkat cells) abrogates the RIP3 up-regulation induces by both TNFa and shikonin in live and dead cells, indicating that necroptosis is in fact induced by both agents. Apoptosis Analysis Cell Line:Jurkat cells Concentration:300 nM Incubation Time:2 hours Result:Increased levels of detectable apoptosis induced by TNFa and shikonin.
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In VivoGSK481 inhibits Ser166 phosphorylation in three mouse RIP1 mutants (IC50=18~110 nM) more potently than in wild-type mouse.
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SynonymsGSK481 | GSK'481
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PathwayApoptosis
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TargetRIP kinase
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RecptorRIP1
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number1622849-58-4
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Formula Weight377.3932
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Molecular FormulaC21H19N3O4
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 35 mg/mL
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SMILESO=C(C1=NOC(CC2=CC=CC=C2)=C1)N[C@H]3COC4=CC=CC=C4N(C)C3=O
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Chemical Name3-Isoxazolecarboxamide, 5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Harris PA, et al. J Med Chem. 2016 Mar 10;59(5):2163-78.
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