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GW 806742X

Chemical Structure : GW 806742X

CAS No.: 579515-63-2

GW 806742X (T0466, GW806742X)

Catalog No.: PC-70325Not For Human Use, Lab Use Only.

GW 806742X (T0446) is a small molecule MLKL (Mixed Lineage Kinase Domain-Like) interactor that binds the MLKL pseudokinase domain (Kd=9.3 uM), retards membrane association to inhibit necroptosis.

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Biological Activity

GW 806742X (T0446) is a small molecule MLKL (Mixed Lineage Kinase Domain-Like) interactor that binds the MLKL pseudokinase domain (Kd=9.3 uM), retards membrane association to inhibit necroptosis.
GW 806742X rescues 50% of wild-type MDFs from TSQ-induced necroptosis with IC50 <50 nM, with >50-fold greater potency than Nec-1.
GW 806742X enhances RIPK3-mediated phosphorylation of MLKL (S345 and S347) at 10 uM.
GW 806742X (T0446) also activates PINK1-Parkin signaling, induces Parkin mitochondrial translocation in dopaminergic neurons differentiated from iPS cells (iPSCs) without obvious ΔΨm reduction and cell toxicity.

Physicochemical Properties

M.Wt 573.551
Formula C25H22F3N7O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-((4-(methyl(4-(3-(4-(trifluoromethoxy)phenyl)ureido)phenyl)amino)pyrimidin-2-yl)amino)benzenesulfonamide

References

1. Hildebrand JM, et al. Proc Natl Acad Sci U S A. 2014 Oct 21;111(42):15072-7.
2. Shiba-Fukushima K, et al. iScience. 2020 May 22;23(5):101048.

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