SKI-178

SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells) . SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines[1][2].

Product Specifications

CAS Number

[1259484-97-3]

UNSPSC

12352005

Hazard Statement

H302, H318

Target

Apoptosis; SphK

Type

Reference compound

Related Pathways

Apoptosis; Immunology/Inflammation

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ski-178.html

Concentration

10mM

Purity

99.29

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(C1=CC(C2=CC=C(OC)C=C2)=NN1)N/N=C(C3=CC=C(OC)C(OC)=C3)\C

Molecular Formula

C21H22N4O4

Molecular Weight

394.42

Precautions

H302, H318

References & Citations

[1]Hengst JA, et al. SKI-178: A Multitargeted Inhibitor of Sphingosine Kinase and Microtubule Dynamics Demonstrating Therapeutic Efficacy in Acute Myeloid Leukemia Models. Cancer Transl Med. 2017;3 (4) :109-121.|[2]Hengst JA, et al. Development of a sphingosine kinase 1 specific small-molecule inhibitor. Bioorg Med Chem Lett. 2010;20 (24) :7498-7502.|[3]Dick TE, et al. The apoptotic mechanism of action of the sphingosine kinase 1 selective inhibitor SKI-178 in human acute myeloid leukemia cell lines. J Pharmacol Exp Ther. 2015;352 (3) :494-508.