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MP A08

Names

[ CAS No. ]:
219832-49-2

[ Name ]:
MP A08

[Synonym ]:
4-Methyl-N-{2-[(E)-(2-{[(4-methylphenyl)sulfonyl]amino}benzylidene)amino]phenyl}benzenesulfonamide
Benzenesulfonamide, 4-methyl-N-[2-[(E)-[[2-[[(4-methylphenyl)sulfonyl]amino]phenyl]imino]methyl]phenyl]-

Biological Activity

[Description]:

MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SphK1 and SphK2 with Kivalues of 6.9 ± 0.8 μM and 27 ± 3 μM, respectively.In vitro:MP-A08 blocks pro-proliferative signalling pathways, induces mitochondrial-associated apoptosis in a SK-dependent manner, and reduces the growth of human lung adenocarcinoma tumours in a mouse xenograft model by both inducing tumour cell apoptosis and inhibiting tumour angiogenesis. MP-A08 inhibit SphK2, cause a decrease in EC barrier integrity in vitro in both cell type.[2]In vivo: MP-A08 suppresses the growth of human lung tumor xenografts in mice.

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> SPHK
Research Areas >> Cancer

[References]

[1]. Pitman MR et al. A selective ATP-competitive sphingosine kinase inhibitor demonstrates anti-cancer properties. Oncotarget, 2015 Mar 30, 6(9):7065-83.

[2]. Dimasi DP et al. Examining the Role of Sphingosine Kinase-2 in the Regulation of Endothelial Cell Barrier Integrity. Microcirculation, 2016 Apr, 23(3):248-65.


[Related Small Molecules]

ABC294640 | K145 (hydrochloride) | SK1-IN-1 | PF-543 (Citrate) | SKI II | MHP

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
717.1±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C27H25N3O4S2

[ Molecular Weight ]:
519.635

[ Flash Point ]:
387.5±35.7 °C

[ Exact Mass ]:
519.128662

[ LogP ]:
5.31

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.634

[ Storage condition ]:
2-8℃

Related Compounds