An inhibitor of SK1 and SK2 (Kis = 27 and 6.9 μM

MP-A08 – 1 mg

Brand:
Cayman
CAS:
219832-49-2
Storage:
-20
UN-No:
Non-Hazardous - /

MP-A08 is an ATP-competitive inhibitor of sphingosine kinases (SKs) 1 and 2 (Kis = 27 and 6.9 μM, respectively).{38144} It is selective for SK1/2 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; Item No. 62570) without inducing degradation of SK1 in Jurkat cells. It induces a 3.7-, 3.5-, and 5.8-fold increase in C-18 ceramide (Item No. 19556), C-20 ceramide (Item No. 10724), 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.  

 

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Description

An inhibitor of SK1 and SK2 (Kis = 27 and 6.9 μM, respectively); selective for SK1/2 over a panel of 140 human protein kinases at concentrations up to 25 μM; reduces generation of cellular S1P without inducing SK1 degradation in Jurkat cells; induces a 3.7-, 3.5-, and 5.8-fold increase in C-18 ceramide, C-20 ceramide, and C20:1-ceramide levels, respectively; reduces proliferation of a variety of human cancer cell lines (EC50s = 8-44.9 μM); reduces tumor vasculature and volume as well as S1P protein levels in A549 human lung adenocarcinoma xenografts in mice,

Formal name: 4-methyl-N-[2-[[[2-[[(4-methylphenyl)sulfonyl]amino]phenyl]imino]methyl]phenyl]-benzenesulfonamide

Synonyms:  NSC 122314

Molecular weight: 519.6

CAS: 219832-49-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Lipid Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Signaling|JNK Signaling||Research Area|Cancer|Cell Signaling|p38 MAPK Signaling||Research Area|Cell Biology|Cell Death|Apoptosis

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