| Identification | Back Directory | [Name]
MP-A08 | [CAS]
219832-49-2 | [Synonyms]
MP-A08
4-Methyl-N-[2-[[[2-[[(4-methylphenyl)sulfonyl]amino]phenyl]imino]methyl]phenyl]benzenesulfonamide
Benzenesulfonamide, 4-methyl-N-[2-[[[2-[[(4-methylphenyl)sulfonyl]amino]phenyl]imino]methyl]phenyl]- | [Molecular Formula]
C27H25N3O4S2 | [MOL File]
219832-49-2.mol | [Molecular Weight]
519.64 |
| Chemical Properties | Back Directory | [Boiling point ]
717.1±70.0 °C(Predicted) | [density ]
1.28±0.1 g/cm3(Predicted) | [solubility ]
DMF: 33 mg/ml; DMF:PBS(pH7.2) (1:2): 0.3 mg/ml; DMSO: 12 mg/ml | [form ]
A crystalline solid | [pka]
7.88±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
MP-A08 is an ATP-competitive inhibitor of sphingosine kinases SPHK1 and SPHK2 (Kis = 27 and 6.9 μM, respectively). It is selective for SPHK1/2 over a panel of 140 human protein kinases at concentrations up to 25 μM. MP-A08 (15 μM) reduces generation of cellular sphingosine-1-phosphate (S1P; ) without inducing degradation of SPHK1 in Jurkat cells. It induces a 3.7-, 3.5-, and 5.8-fold increase in C-18 ceramide , C-20 ceramide , and C20:1-ceramide levels, respectively, and dose-dependently activates the apoptosis-associated p38 and JNK pathways in vitro. MP-A08 reduces proliferation of a variety of human cancer cell lines (EC50s = 8-44.9 μM). MP-A08 also reduces tumor vasculature, as determined by CD31 staining, and volume as well as S1P protein levels in A549 human lung adenocarcinoma xenografts in mice. | [Uses]
NSC 122314 is selective ATP competitive sphingosine kinase 2 and 1 inhibitor. Also it induces mitochondrial-associated apoptosis. | [Definition]
ChEBI: MP-A08 is a sulfonamide that consists of two moieties of 4-methyl-N-phenylbenzenesulfonamide connected to each other at position 2 by an aldimine linker. It is a ATP-competitive inhibitor of sphingosine kinase that targets both SK1 and SK2 (Ki values of 27 muM and 6.9 muM, respectively) and exhibits anti-cancer properties. It has a role as an antineoplastic agent, an apoptosis inducer, an angiogenesis inhibitor and an EC 2.7.1.91 (sphingosine kinase) inhibitor. It is a sulfonamide, a member of toluenes and an aldimine. | [in vivo]
MP-A08 suppresses the growth of human lung tumor xenografts in mice. | [IC 50]
SphK1 | [storage]
Store at -20°C |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
DC Chemicals
|
| Tel: |
021-58447131 13564518121 |
| Website: |
http://m.is0513.com/ShowSupplierProductsList927327/0.htm |
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