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GSK'872 RIP kinase inhibitor

Name: GSK'872
Brand: Selleck Chemicals
SKU: S8465
Availability: InStock
Rating: 5 (93 reviews)

Cat.No.S8465

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.

Chemical Structure

Molecular Weight: 383.49

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Apoptosis related Ras STAT TNF-alpha Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 c-RET MDM2/MDMX Myc IAP OXPHOS PERK Thymidylate Synthase FKBP Heme Oxygenase PFKFB PKD Survivin Pyroptosis ASK Bcl-6 Nur77 DAPK TRADD cytohesin TACE Cuproptosis
Related Products	Necrostatin-1 (Nec-1) Necrostatin 2 racemate (Nec-1s) Mito-TEMPO RIPA-56 GSK2982772 GSK'963 GSK583 GSK2983559 (compound 3) Resibufogenin GSK'547 ICCB-19 hydrochloride HS-1371 GSK481

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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

Chemical Information, Storage & Stability

Molecular Weight	383.49	Formula	C₁₉H₁₇N₃O₂S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1346546-69-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GSK2399872A			Smiles	CC(C)S(=O)(=O)C1=CC2=C(C=CN=C2C=C1)NC3=CC4=C(C=C3)SC=N4

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.850mg/ml (10.04mM)	Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 77 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (6.52mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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. This compound 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. It also blocks necroptosis in primary human neutrophils isolated from whole blood. This chemical inhibits TLR3- or DAI-induced death, two RIP1-independent pathways of necroptosis. It induces caspase activation followed by apoptotic cell death^[1].
In vivo	GSK'872 treatment significantly decreases HIF-1α expression compared with no treatment after ischemia injury in vivo^[3].
References	https://pubmed.ncbi.nlm.nih.gov/25459880/ https://pubmed.ncbi.nlm.nih.gov/24019532/ https://pubmed.ncbi.nlm.nih.gov/28724891/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Rip1 / Rip3 / p-MLKL / MLKL		31214277
Growth inhibition assay	Cell viability		24019532

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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