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
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
N-Bromosuccinimide Price
- Product number
- KIN0008618
- Product name
- GSK-840
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $458.27
- Updated
- 2021/12/16
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
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