SKI-178

• Description:

  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].

• 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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C, 3 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  SphK1; SphK2

• CAS Number:

  [1259484-97-3]