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GW806742X (hydrochloride)

GW806742X hydrochloride, 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 hydrochloride has activity against VEGFR2 (IC50=2 nM) . GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis[1][2].

Product Specifications

UNSPSC

12352005

Target

Mixed Lineage Kinase; VEGFR

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

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

Purity

98.30

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic)

Smiles

[H]Cl.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

C25H23ClF3N7O4S

Molecular Weight

610.01

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;111 (42) :15072-15077.|[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

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

VEGFR2/KDR/Flk-1

Citation 01

Nature. 2023 Mar;615 (7950) :158-167.|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.

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