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GSK963

Catalog No. T5054 CAS 2049868-46-2

Synonyms: GSK963 (Racemate)

GSK963 (Racemate), a structurally distinct, potent and selective inhibitor of RIP1 kinase(IC50=29 nM).

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GSK963, CAS 2049868-46-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 43.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 247.00
50 mg	In stock	$ 397.00
100 mg	In stock	$ 582.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 98.68%

Biological Description

Chemical Properties

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Description	GSK963 (Racemate), a structurally distinct, potent and selective inhibitor of RIP1 kinase(IC50=29 nM).
Targets&IC50	RIP1:29 nM
In vitro	The increased potency of GSK 963 relative to Nec-1 in vitro also translated into increased efficacy in the TNF+zVAD-induced model of sterile shock.?At a dose of 2 mg/kg, GSK 963 was able to completely inhibit temperature loss in response to TNF+zVAD, ?the phenotype of the recently described RIP1 kinase-dead knock-in mice.?The level of inhibition of temperature loss in this acute model at different doses of GSK 963 was in line with the predictions of efficacy based on modeling of the pharamacokinetic profile and in vitro potency of GSK 963.
In vivo	GSK 963 efficiently blocked necroptosis in both murine and human cells with IC50 values of 1 nM and 4 nM, respectively, whereas the inactive analog GSK 962 was at least 1000-fold less potent in these assays.
Kinase Assay	GSK′963 was tested against 339 kinases using a P33-radiolabeled assay at Reaction Corp Biology. The compound was tested at a single dose in duplicate at 10?μM. Reactions were carried out at 10?μM ATP. Data are reported as % enzyme activity (relative to DMSO controls).

Synonyms	GSK963 (Racemate)
Molecular Weight	230.31
Formula	C14H18N2O
CAS No.	2049868-46-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 40 mg/mL (173.67 mM)

References and Literature

1. Berger SB, et al. Characterization of GSK'963: a structurally distinct, potent and selective inhibitor of RIP1 kinase. Cell Death Discov. 2015 Jul 27;1:15009.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Pyroptosis Compound Library Kinase Inhibitor Library HIF-1 Signaling Pathway Compound Library Bioactive Compound Library Anti-Ovarian Cancer Compound Library Bioactive Compounds Library Max Immuno-Oncology Compound Library Anti-Liver Cancer Compound Library

Related Products

Related compounds with same targets

Necrostatin-1 RIPK2/3-IN-1 GSK-872 GSK872 HCl（1346546-69-7 free base） GSK3145095 Necrostatin-34 RIPK1-IN-9 RIP1 kinase inhibitor 6

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Keywords

GSK963 2049868-46-2 Apoptosis NF-Κb RIP kinase GSK 963 Inhibitor Receptor-interacting protein kinases inhibit RIPK GSK963 (Racemate) GSK-963 Racemate inhibitor

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