Home Apoptosis RIP kinase inhibitor GSK'872 For research use only.

GSK'872

Synonyms: GSK2399872A

GSK'872 is a potent and selective RIP3 kinase 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.

GSK'872 Chemical Structure

GSK'872 Chemical Structure

CAS No. 1346546-69-7

Purity & Quality Control

GSK'872 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
K562  Function assay 1 h GSK'872 significantly inhibited cell death 29527209
HBE cells Function assay 5 μM GSK'872 treatment significantly reduced the particulate matter (PM)-induced expression of IL6 and IL8 at both mRNA and protein levels 29621753
U251 Function assay 5 μM 1 h effectively decreased TP4-mediated cytotoxicity 30717309
U87MG Function assay 5 μM 1 h effectively decreased TP4-mediated cytotoxicity 30717309
HT-22 Function assay 0.1, 1 and 10 μM 9 h zVAD, GSK’872 and combinative intervention alleviated morphologic alterations and attenuated cell death induced by oxygen-glucose deprivation and reoxygenation 28724891
MPSC1 cells Cell viability assay 6 μM 2 h pre-treatment for 2 h with GSK'872 partially reversed CD40L-induced reductions in cell viability 26313915
Click to View More Cell Line Experimental Data

Biological Activity

Description GSK'872 is a potent and selective RIP3 kinase 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
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[1].
Cell Research Cell lines 3T3-SA cells
Concentrations 0.3, 1, 3 μM
Incubation Time 18 h
Method

Viability of 3T3-SA cells at 18 h after treatment with TNF in the presence of Z-VAD-fmk in vehicle control (DMSO) or treated with the indicated concentrations of RIP3 kinase inhibitors, GSK'843 or GSK'872 are assayed.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Rip1 / Rip3 / p-MLKL / MLKL 31214277
Growth inhibition assay Cell viability 24019532
In Vivo
In vivo GSK'872 treatment significantly decreases HIF-1α expression compared with no treatment after ischemia injury in vivo[3].
Animal Research Animal Models C57BL/6 mice
Dosages 1.9 mmol/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 383.49 Formula

C19H17N3O2S2
CAS No. 1346546-69-7 SDF Download GSK'872 SDF
Smiles CC(C)S(=O)(=O)C1=CC2=C(C=CN=C2C=C1)NC3=CC4=C(C=C3)SC=N4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 76 mg/mL ( (198.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 40 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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