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GW806742X

GW806742X, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X has activity against VEGFR2 (IC50=2 nM) . GW806742X retards MLKL membrane translocation and inhibits necroptosis[1][2].

Product Specifications

CAS Number

[579515-63-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Mixed Lineage Kinase; VEGFR

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK

Field of Research

Others

Assay Protocol

https://www.medchemexpress.com/gw806742x.html

Purity

99.91

Solubility

DMSO : 100 mg/mL (ultrasonic)

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

Molecular Formula

C25H22F3N7O4S

Molecular Weight

573.55

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

VEGFR2/KDR/Flk-1

Citation 01

Acta Histochem. 2022 May;124 (4) :151875.|Acta Pharmacol Sin. 2022 May;43 (5) :1324-1336.|Autophagy. 2022 Apr;18 (4) :726-744.|bioRxiv. 2023 Apr 25.|Cell Death Dis. 2025 Aug 29;16 (1) :657.|Cell Death Discov. 2024 Mar 8;10 (1) :122.|Curr Protoc. 2024 Jul;4 (7) :e1112.|EMBO Mol Med. 2025 Apr;17 (4) :679-695.|Exp Gerontol. 2024 May:189:112401.|Inflammation. 2025 Apr 7.|Int Immunopharmacol. 2025 Sep 3:165:115427.|Int J Mol Sci. 2023 May 11;24 (10) :8609.|J Clin Invest. 2025 May 13:e188541.|J Hazard Mater. 2024 Apr 5:467:133719.|J Immunol. 2025 Jun 1;214 (6) :1236-1246.|Microbiol Spectr. 2022 Aug 31;10 (4) :e0104522.|Nat Commun. 2024 Jul 18;15 (1) :6043.|PLoS Pathog. 2025 May 13;21 (5) :e1013167.|Transbound Emerg Dis. 2025 Oct 7:2025:8510846.|Viruses. 2023 Oct 24;15 (11) :2141.|Nature. 2023 Mar;615 (7950) :158-167.

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