WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 408128
CAS#: 579515-63-2
Description: GW806742X is a potent MLKL inhibitor, also a human and murine necroptosis inhibitor. GW806742X binds the MLKL pseudokinase domain with a Kd value of 9.3 μM and has anti-necroptosis activity. GW806742X has activity against VEGFR2. GW806742X blocked necroptosis and IL-33 release in vitro and reduced eosinophilia in Aspergillus fumigatus extract-induced asthma in vivo, an allergic inflammation model that is highly dependent on IL-33.
MedKoo Cat#: 408128
Name: GW806742X
CAS#: 579515-63-2
Chemical Formula: C25H22F3N7O4S
Exact Mass: 573.1406
Molecular Weight: 573.5512
Elemental Analysis: C, 52.35; H, 3.87; F, 9.94; N, 17.10; O, 11.16; S, 5.59
Synonym: GW806742X; GW-806742X; GW 806742X;
IUPAC/Chemical Name: 3-(4-(Methyl(4-(3-(4-(trifluoromethoxy)phenyl)ureido)phenyl)amino)pyrimidin-2-ylamino)benzenesulfonamide
InChi Key: SNRUTMWCDZHKKM-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H22F3N7O4S/c1-35(22-13-14-30-23(34-22)31-18-3-2-4-21(15-18)40(29,37)38)19-9-5-16(6-10-19)32-24(36)33-17-7-11-20(12-8-17)39-25(26,27)28/h2-15H,1H3,(H2,29,37,38)(H,30,31,34)(H2,32,33,36)
SMILES Code: 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
1: Moreira-Nunes CA, Mesquita FP, Portilho AJS, Mello Júnior FAR, Maués JHDS, Pantoja LDC, Wanderley AV, Khayat AS, Zuercher WJ, Montenegro RC, de Moraes- Filho MO, de Moraes MEA. Targeting aurora kinases as a potential prognostic and therapeutical biomarkers in pediatric acute lymphoblastic leukaemia. Sci Rep. 2020 Dec 4;10(1):21272. doi: 10.1038/s41598-020-78024-8. PMID: 33277547; PMCID: PMC7718893.
2: Shlomovitz I, Erlich Z, Speir M, Zargarian S, Baram N, Engler M, Edry-Botzer L, Munitz A, Croker BA, Gerlic M. Necroptosis directly induces the release of full-length biologically active IL-33 in vitro and in an inflammatory disease model. FEBS J. 2019 Feb;286(3):507-522. doi: 10.1111/febs.14738. Epub 2019 Jan 4. PMID: 30576068.
3: Lusthaus M, Mazkereth N, Donin N, Fishelson Z. Receptor-Interacting Protein Kinases 1 and 3, and Mixed Lineage Kinase Domain-Like Protein Are Activated by Sublytic Complement and Participate in Complement-Dependent Cytotoxicity. Front Immunol. 2018 Feb 23;9:306. doi: 10.3389/fimmu.2018.00306. PMID: 29527209; PMCID: PMC5829068.
4: González-Juarbe N, Gilley RP, Hinojosa CA, Bradley KM, Kamei A, Gao G, Dube PH, Bergman MA, Orihuela CJ. Pore-Forming Toxins Induce Macrophage Necroptosis during Acute Bacterial Pneumonia. PLoS Pathog. 2015 Dec 11;11(12):e1005337. doi: 10.1371/journal.ppat.1005337. PMID: 26659062; PMCID: PMC4676650.
