SKI-I

Names

[ CAS No. ]:
306301-68-8

[ Name ]:
SKI-I

[Synonym ]:
Sphingosine Kinase Inhibitor, SKI-I
5-naphthalen-2-yl-1H-pyrazol-3-carboxylic acid (2-hydroxynaphthalen-1-ylmethylene)-hydrazide

Biological Activity

[Description]:

SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines[1][2].

[Related Catalog]:

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

[Target]

IC50: 1.2 μM (ST-hSK); 11 μM (hERK2)[1]


[In Vitro]

SKI-I (Compound I; 5 μg/mL) inhibits SK activity by 99%[1]. SKI-I (10 μM; 24 h) induces the apoptosis of T24 cells[1].

[References]

[1]. French KJ, et, al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9.

[2]. Sharma AK, et, al. Synthesis and bioactivity of sphingosine kinase inhibitors and their novel aspirinyl conjugated analogs. Eur J Med Chem. 2010 Sep;45(9):4149-56.

Chemical & Physical Properties

[ Molecular Formula ]:
C25H18N4O2

[ Molecular Weight ]:
406.43600

[ Exact Mass ]:
406.14300

[ PSA ]:
90.37000

[ LogP ]:
5.24350

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds