An inhibitor of SPHK1 and SPHK2
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MP-A08

Item No. 21903

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-methyl-N-[2-[[[2-[[(4-methylphenyl)sulfonyl]amino]phenyl]imino]methyl]phenyl]-benzenesulfonamide
CAS Number
219832-49-2
Synonyms
  • NSC 122314
Molecular Formula
C27H25N3O4S2
Formula Weight
519.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS(pH7.2) (1:2): 0.3 mg/mlDMSO: 10 mg/ml
λmax
225 nm
SMILES
CC1=CC=C(S(NC2=CC=CC=C2/C=N/C3=C(NS(C4=CC=C(C)C=C4)(=O)=O)C=CC=C3)(=O)=O)C=C1
InChi Code
InChI=1S/C27H25N3O4S2/c1-20-11-15-23(16-12-20)35(31,32)29-25-8-4-3-7-22(25)19-28-26-9-5-6-10-27(26)30-36(33,34)24-17-13-21(2)14-18-24/h3-19,29-30H,1-2H3/b28-19+
InChi Key
FLDBNMYJUMAXDQ-TURZUDJPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $37

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    5 mg

    $106

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    10 mg

    $194

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    25 mg

    $436

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    Product Description

    MP-A08 is an ATP-competitive inhibitor of sphingosine kinases SPHK1 and SPHK2 (Kis = 27 and 6.9 μM, respectively).1 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; Item No. 62570) without inducing degradation of SPHK1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pitman, M.R., Powell, J.A., Coolen, C., et al. A selective ATP-competitive sphingosine kinase inhibitor demonstrates anti-cancer properties. Oncotarget 6(9), 7065-7083 (2015).