[CAS NO. 1346546-69-7] GSK'872 (GSK2399872A)
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PRODUCTS SPECIFICATIONS [1346546-69-7]
Catelog
SLK-S8465
Brand
Selleck
CAS
1346546-69-7
DESCRIPTION [1346546-69-7]
Overview
| MDL | MFCD30481302 |
|---|---|
| Molecular Weight | 383.49 |
| Molecular Formula | C19H17N3O2S2 |
| SMILES | O=S(C1=CC=C2N=CC=C(NC3=CC=C(SC=N4)C4=C3)C2=C1)(C(C)C)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6076 mL | 13.0381 mL | 26.0763 mL |
| 5 mM | 0.5215 mL | 2.6076 mL | 5.2153 mL |
| 10 mM | 0.2608 mL | 1.3038 mL | 2.6076 mL |
| 50 mM | 0.0522 mL | 0.2608 mL | 0.5215 mL |
Description
GSK'872 (GSK2399872A) is a potent and selective inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.
Targets
| RIP3K [1] (Cell-free assay) |
| 1.3 nM |
In vitro
When assayed at 1 μM, GSK'872 fails to inhibit most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase when tested directly. GSK'872 blocks TNF-induced necroptosis in a concentration-dependent manner in HT-29 cells. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK'872 also blocks necroptosis in primary human neutrophils isolated from whole blood. GSK'872 inhibits TLR3- or DAI-induced death, two RIP1-independent pathways of necroptosis. It induces caspase activation followed by apoptotic cell death.
In vivo
GSK'872 treatment significantly decreases HIF-1α expression compared with no treatment after ischemia injury in vivo.
References
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