ChemicalBook--->CAS DataBase List--->2361146-30-5

2361146-30-5

2361146-30-5 Structure

2361146-30-5 Structure
IdentificationBack Directory
[Name]

GSK840
[CAS]

2361146-30-5
[Synonyms]

GSK840
tert-butyl 2-(4-(5-(methylcarbamoyl)-1H-benzo[d]imidazol-1-yl)phenyl)acetate
[Molecular Formula]

C21H23N3O3
[MOL File]

2361146-30-5.mol
[Molecular Weight]

365.43
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

110 mg/mL in DMSO
Spectrum DetailBack Directory
[Spectrum Detail]

GSK840(2361146-30-5)1HNMR
Hazard InformationBack Directory
[Biological Activity]

GSK840 is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, binds with high affinity to the RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM.
[in vitro]

GSK840 (GSK'840) (0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in a concentration-dependent manner.
GSK840 binds the kinase domain and inhibits kinase activity with high specificity, targeting a broader range of pro-necrotic stimuli than can be achieved with RIP1 kinase inhibitors.

Cell Viability Assay

Cell Line: Human HT-29 cells (TNF 10 ng/ml + zVAD-fmk 20 μM + SMAC007 100 nM)
Concentration: 0.01-3 μM
Incubation Time: 24 hours
Result: Blocked TNF-induced necroptosis in a concentration-dependent manner.
[target]

IC50: 0.3 nM (RIP3)

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