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Chemical Structure| 579515-63-2 Chemical Structure| 579515-63-2

Structure of GW806742X
CAS No.: 579515-63-2

Chemical Structure| 579515-63-2

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GW806742X, an ATP analog, is a potent MLKL inhibitor that binds to the MLKL pseudokinase domain with a Kd value of 9.3μM. GW806742X has anti-VEGFR2 activity (IC50=2 nM). GW806742X delays MLKL membrane displacement and inhibits necrosis.

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Product Details of GW806742X

CAS No. :579515-63-2
Formula : C25H22F3N7O4S
M.W : 573.55
SMILES Code : O=C(NC1=CC=C(OC(F)(F)F)C=C1)NC2=CC=C(C=C2)N(C)C3=NC(NC4=CC(S(=O)(N)=O)=CC=C4)=NC=C3
MDL No. :MFCD29036385
InChI Key :SNRUTMWCDZHKKM-UHFFFAOYSA-N
Pubchem ID :5329829

Safety of GW806742X

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of GW806742X

RTK
MAPK

Isoform Comparison

Biological Activity

Target
  • MLKL

    MLKL, Kd:9.3 μM

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.74mL

0.35mL

0.17mL

8.72mL

1.74mL

0.87mL

17.44mL

3.49mL

1.74mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

[1]Hildebrand JM, Tanzer MC, Lucet IS, Young SN, Spall SK, Sharma P, Pierotti C, Garnier JM, Dobson RC, Webb AI, Tripaydonis A, Babon JJ, Mulcair MD, Scanlon MJ, Alexander WS, Wilks AF, Czabotar PE, Lessene G, Murphy JM, Silke J. 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. doi: 10.1073/pnas.1408987111. Epub 2014 Oct 6. PMID: 25288762; PMCID: PMC4210347.

[2]Sammond DM, Nailor KE, Veal JM, Nolte RT, Wang L, Knick VB, Rudolph SK, Truesdale AT, Nartey EN, Stafford JA, Kumar R, Cheung M. Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3519-23. doi: 10.1016/j.bmcl.2005.05.096. PMID: 15990302.

[3] Andre L Samson,et al. MLKL trafficking and accumulation at the plasma membrane control the kinetics and threshold for necroptosis. Nat Commun. 2020 Jun 19;11(1):3151.

[4]Jialin Dai,et al. A necroptotic-independent function of MLKL in regulating endothelial cell adhesion molecule expression. Cell Death Dis. 2020 Apr 24;11(4):282.

[5] Bingqing Xia,et al. MLKL forms cation channels. Cell Res. 2016 May;26(5):517-28.

[6]Sevda Lule,et al. Cell-specific activation of RIPK1 and MLKL after intracerebral hemorrhage in mice. J Cereb Blood Flow Metab. 2021 Jul;41(7):1623-1633.

[7]Kimberley D Gutierrez,et al. MLKL Activation Triggers NLRP3-Mediated Processing and Release of IL-1β Independently of Gasdermin-D. J Immunol. 2017 Mar 1;198(5):2156-2164.

[8] 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.

 

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