ChemicalBook > CAS DataBase List > GSK840

GSK840

Product Name
GSK840
CAS No.
2361146-30-5
Chemical Name
GSK840
Synonyms
GSK840;tert-butyl2-(4-(5-(methylcarbamoyl)-1H-benzo[d]im;tert-butyl 2-(4-(5-(methylcarbamoyl)-1H-benzo[d]imidazol-1-yl)phenyl)acetate;Inhibitor,RIP kinase,GSK 840,Receptor-interacting protein kinases,GSK840,inhibit,GSK-840,RIPK;Benzeneacetic acid, 4-[5-[(methylamino)carbonyl]-1H-benzimidazol-1-yl]-, 1,1-dimethylethyl ester
CBNumber
CB95419747
Molecular Formula
C21H23N3O3
Formula Weight
365.43
MOL File
2361146-30-5.mol
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GSK840 Property

Density 
1.18±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
110 mg/mL in DMSO
form 
Solid
pka
14.16±0.46(Predicted)
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

American Custom Chemicals Corporation
Product number
KIN0008618
Product name
GSK-840
Purity
95.00%
Packaging
5MG
Price
$458.27
Updated
2021/12/16
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GSK840 Chemical Properties,Usage,Production

Uses

GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM[1].

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)

References

[1] Mandal P, et al. RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol Cell. 2014 Nov 20;56(4):481-95. DOI:10.1016/j.molcel.2014.10.021

GSK840 Preparation Products And Raw materials

Raw materials

Preparation Products

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2361146-30-5, GSK840Related Search:


  • GSK840
  • tert-butyl 2-(4-(5-(methylcarbamoyl)-1H-benzo[d]imidazol-1-yl)phenyl)acetate
  • Inhibitor,RIP kinase,GSK 840,Receptor-interacting protein kinases,GSK840,inhibit,GSK-840,RIPK
  • tert-butyl2-(4-(5-(methylcarbamoyl)-1H-benzo[d]im
  • Benzeneacetic acid, 4-[5-[(methylamino)carbonyl]-1H-benzimidazol-1-yl]-, 1,1-dimethylethyl ester
  • 2361146-30-5