Art. -Nr.: HY-112292

GW806742X

25 Cited Publications

Kundenbewertung

Based on 25 publication(s) in Google Scholar

GW806742X, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a K_d of 9.3 μM. GW806742X has activity against VEGFR2 (IC₅₀=2 nM). GW806742X retards MLKL membrane translocation and inhibits necroptosis.

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Reinheit: 99.38%
CAS. Nr.: 579515-63-2
Formel: C₂₅H₂₂F₃N₇O₄S
Molecular Weight:573.55

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GW806742X Chemical Structure

CAS. Nr.: 579515-63-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (25)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]

MLKL

9.3 μM (Kd)

VEGFR2

2 nM (IC₅₀)

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Fibroblast	IC₅₀	<50 nM Compound: 42	Anti-necroptotic activity in mouse dermal fibroblast assessed as inhibition in T/S/Q induced necroptosis measured by flow cytometry Anti-necroptotic activity in mouse dermal fibroblast assessed as inhibition in T/S/Q induced necroptosis measured by flow cytometry	[PMID: 36781172]
Fibroblast	IC₅₀	<50 nM Compound: 69; GW806742X	Anti-neprotic activity in mouse fibroblasts cells Anti-neprotic activity in mouse fibroblasts cells	[PMID: 31622096]
HUVEC	IC₅₀	5 nM Compound: 23	Inhibitory concentration against human umbilical vein endothelial cells (HUVECs) induced by VEGF Inhibitory concentration against human umbilical vein endothelial cells (HUVECs) induced by VEGF	[PMID: 15990302]
Jurkat	EC₅₀	1.85 μM Compound: 42	Anti-necroptotic activity in FADD-deficient human Jurkat cells assessed as reduction in cell growth preincubated for 30 mins followed by TNFalpha stimulation incubated overnight by CellTiter-Glo assay Anti-necroptotic activity in FADD-deficient human Jurkat cells assessed as reduction in cell growth preincubated for 30 mins followed by TNFalpha stimulation incubated overnight by CellTiter-Glo assay	[PMID: 36781172]

In Vitro

GW806742X (0.1-10000 nM) inhibits necroptotic death of wild-type mouse dermal fibroblasts (MDFs) stimulated with TSQ (1 ng/mL TNF, 500 nM compound A (Smac mimetic), 10 μM Q-VD-OPh) in a dose-dependent manner^[1].
GW806742X shows inhibition of VEGF induced proliferation of HUVECs with an IC50 of 5 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 579515-63-2
Appearance Solid
Molecular Weight 573.55
Formel C₂₅H₂₂F₃N₇O₄S
Color White to off-white
SMILES

O=S(C1=CC=CC(NC2=NC=CC(N(C)C3=CC=C(NC(NC4=CC=C(OC(F)(F)F)C=C4)=O)C=C3)=N2)=C1)(N)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (25)

All Cell Proliferation/Viability AssayWBIHCIn Vivo Imaging

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Journal Impact Factor

Nature

Targeting TBK1 to overcome resistance to cancer immunotherapy. [Abstract]

2023 Mar;615(7950):158-167. PMID: 36634707

GW806742X purchased from MedChemExpress. Usage Cited in: Nature. 2023 Mar;615(7950):158-167. [Abstract]

Cell viability assessment in Tbk1-null B16 cells pre-treated with RIPK3 inhibitor (HS-1371, 2 μM) or MLKL inhibitor (GW806742X, 5 μM) and the pan-caspase inhibitor Q-VD-Oph (20 μM) +/− TNFα/IFNγ for 9 days (n=6, 2 independent experiments: 2-way ANOVA, Dunnett’s multiple comparisons test).
Nat Commun

Necroptosis enhances 'don't eat me' signal and induces macrophage extracellular traps to promote pancreatic cancer liver metastasis. [Abstract]

2024 Jul 18;15(1):6043. PMID: 39025845

GW806742X purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 18;15(1):6043. [Abstract]

WB analysis of necroptosis markers after 48 h treatment with different necroptosis inhibitors. The inhibitors used were Nec-1 (50 µM, a RIPK1 inhibitor), GSK-872 (3 µM, a RIPK3 inhibitor), and GW806742X (1 µM, an MLKL inhibitor).

GW806742X purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 18;15(1):6043. [Abstract]

WB analysis of PCNA in cells untreated/treated with GW806742X (1 µM) for 48 h.

GW806742X purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 18;15(1):6043. [Abstract]

CD47 IHC staining of primary tumours from C57BL/6 orthotopic model received different treatments: saline, anti-mouse IL6 (200 µg, iv., 3×/week), or GW806742X (100 µM in 50 µl, iv., 3×/week); mice were euthanized 4 weeks after injection.

GW806742X purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 18;15(1):6043. [Abstract]

Bioluminescence of total tumour burden in C57BL/6 orthotopic model received different treatments: saline, GW806742X (100 µM in 50 µl, iv., 3×/week), anti-mCD47 (400 µg, ip., 3×/week) or both since day 7 after injection (106 KPC OE-MLKL cells); Images were collected at four weeks after injection; (8 mice per group).
Cell Death Differ

RIPK3 sequentially recruits MLKL and RIPK1 to induce PANoptosis and chemokine production. [Abstract]

2026 Apr 4. PMID: 41935203
Cell Death Differ

Phagocytosis of necroptotic cells optimizes type 1 conventional dendritic cells for induction of a cytotoxic T-cell response. [Abstract]

2026 Feb 28. PMID: 41764333
Autophagy

CAMK2/CaMKII activates MLKL in short-term starvation to facilitate autophagic flux. [Abstract]

2022 Apr;18(4):726-744. PMID: 34282994

GW806742X purchased from MedChemExpress. Usage Cited in: Autophagy. 2022 Apr;18(4):726-744. [Abstract]

Western blots for levels of p-MLKL and MLKL in wild type (WT) L929 cells untreated or treated with either TSZ for 6 h or ECS for 3 h. GW806742X (GW, 1 µM) was included in some samples as indicated 0.5 h before and during the treatment.
J Clin Invest

Activation of intestinal endogenous retroviruses by alcohol exacerbates liver disease. [Abstract]

2025 May 13:e188541. PMID: 40359032
J Hazard Mater

Sodium sulfite triggered hepatic apoptosis, necroptosis, and pyroptosis by inducing mitochondrial damage in mice and AML-12 cells. [Abstract]

2024 Apr 5:467:133719. PMID: 38335615
Cell Death Dis

DJ-1 counteracts Caveolin-1-mediated necroptosis to inhibit epithelial barrier dysfunction in colitis. [Abstract]

2025 Aug 29;16(1):657. PMID: 40877233
Acta Pharmacol Sin

Gout-associated monosodium urate crystal-induced necrosis is independent of NLRP3 activity but can be suppressed by combined inhibitors for multiple signaling pathways. [Abstract]

2022 May;43(5):1324-1336. PMID: 34376811
EMBO Mol Med

Deubiquitination of RIPK3 by OTUB2 potentiates neuronal necroptosis after ischemic stroke. [Abstract]

2025 Apr;17(4):679-695. PMID: 40021931
Cell Death Discov

Bacillus cereus cereolysin O induces pyroptosis in an undecapeptide-dependent manner. [Abstract]

2024 Mar 8;10(1):122. PMID: 38458999
Cell Rep

ISG15 negatively regulates RIPK3-mediated cell death and viral pathogenesis. [Abstract]

2026 May 26;45(5):117360. PMID: 42139056
Inflammation

MLKL-Mediated Necroptosis Predominantly Contributes to Immune-Associated Myocardial Damage. [Abstract]

2025 Apr 7. PMID: 40195182
PLoS Pathog

Caspase-1-licensed pyroptosis drives dsRNA-mediated necroptosis and dampens host defense against bacterial pneumonia. [Abstract]

2025 May 13;21(5):e1013167. PMID: 40359428
Int J Mol Sci

Mitochondrial Trafficking of MLKL, Bak/Bax, and Drp1 Is Mediated by RIP1 and ROS which Leads to Decreased Mitochondrial Membrane Integrity during the Hyperglycemic Shift to Necroptosis. [Abstract]

2023 May 11;24(10):8609. PMID: 37239951
Int Immunopharmacol

Leptin aggravates house dust mite-induced airway inflammation by accelerating macrophage necroptosis. [Abstract]

2025 Sep 3:165:115427. PMID: 40907335
Exp Gerontol

Endoplasmic reticulum stress-induced necroptosis promotes cochlear inflammation: Implications for age-related hearing loss. [Abstract]

2024 May:189:112401. PMID: 38490286
Microbiol Spectr

Enterococcus faecalis-Induced Macrophage Necroptosis Promotes Refractory Apical Periodontitis. [Abstract]

2022 Aug 31;10(4):e0104522. PMID: 35708336
Viruses

ZBP1 Drives IAV-Induced NLRP3 Inflammasome Activation and Lytic Cell Death, PANoptosis, Independent of the Necroptosis Executioner MLKL. [Abstract]

2023 Oct 24;15(11):2141. PMID: 38005819
J Immunol

Innate immune sensor NLRP3 drives PANoptosome formation and PANoptosis. [Abstract]

2025 Jun 1;214(6):1236-1246. PMID: 40249072
Transbound Emerg Dis

Activation of ZBP1/RIPK3/MLKL-Dependent Necroptosis by Pseudorabies Virus Restricts Viral Infection in BV2 Microglia Cells. [Abstract]

2025 Oct 7:2025:8510846. PMID: 41098523
Acta Histochem

Cholecalciferol pretreatment ameliorates ischemia/reperfusion-induced acute kidney injury through inhibiting ROS production, NF-κB pathway and pyroptosis. [Abstract]

2022 May;124(4):151875. PMID: 35334282
Curr Protoc

Defining PANoptosis: Biochemical and Mechanistic Evaluation of Innate Immune Cell Death Activation. [Abstract]

2024 Jul;4(7):e1112. PMID: 39073015
bioRxiv

2026 Jan 25.
bioRxiv

2023 Apr 25.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (174.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7435 mL

8.7176 mL

17.4353 mL

5 mM

0.3487 mL

1.7435 mL

3.4871 mL

10 mM

0.1744 mL

0.8718 mL

1.7435 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hildebrand JM, et al. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. Proc Natl Acad Sci U S A. 2014 Oct 21;111(42):15072-7. [Content Brief]

[2]. Sammond DM, et al. Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase. Bioorg Med Chem Lett. 2005;15(15):3519-3523. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7435 mL	8.7176 mL	17.4353 mL	43.5882 mL
	5 mM	0.3487 mL	1.7435 mL	3.4871 mL	8.7176 mL
	10 mM	0.1744 mL	0.8718 mL	1.7435 mL	4.3588 mL
	15 mM	0.1162 mL	0.5812 mL	1.1624 mL	2.9059 mL
	20 mM	0.0872 mL	0.4359 mL	0.8718 mL	2.1794 mL
	25 mM	0.0697 mL	0.3487 mL	0.6974 mL	1.7435 mL
	30 mM	0.0581 mL	0.2906 mL	0.5812 mL	1.4529 mL
	40 mM	0.0436 mL	0.2179 mL	0.4359 mL	1.0897 mL
	50 mM	0.0349 mL	0.1744 mL	0.3487 mL	0.8718 mL
	60 mM	0.0291 mL	0.1453 mL	0.2906 mL	0.7265 mL
	80 mM	0.0218 mL	0.1090 mL	0.2179 mL	0.5449 mL
	100 mM	0.0174 mL	0.0872 mL	0.1744 mL	0.4359 mL

Keywords

GW806742X

25 Cited Publications

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GW806742X

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Cell Death Inhibitor Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GW806742X

Alle VEGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (25)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GW806742X Related Classifications

HY-112292 Related Classifications