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SKI-178

Catalog No. T9014   CAS 1259484-97-3

SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1.

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SKI-178 Chemical Structure
SKI-178, CAS 1259484-97-3
Pack Size Availability Price/USD Quantity
2 mg In stock $ 41.00
5 mg In stock $ 66.00
10 mg In stock $ 116.00
25 mg In stock $ 226.00
50 mg In stock $ 363.00
100 mg In stock $ 547.00
500 mg In stock $ 1,170.00
1 mL * 10 mM (in DMSO) In stock $ 73.00
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Purity: 99.2%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1.
Targets&IC50 SPHK1:0.1-1.8 μM
In vitro SKI-178 is a multi-targeted agent that functions both as an inhibitor of the SphKs as well as a disruptor of the microtubule network.?SKI-178 induced apoptosis arises from a synergistic interaction of these two activities.?SKI-178 is safe and effective in mouse models of AML, supporting its further development as a multi-targeted anti-cancer therapeutic agent[1].
Molecular Weight 394.42
Formula C21H22N4O4
CAS No. 1259484-97-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (126.77 mM), Sonification is recommended.

TargetMolReferences and Literature

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. 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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library GPCR Compound Library Kinase Inhibitor Library Bioactive Compounds Library Max Anti-Cancer Compound Library NO PAINS Compound Library Bioactive Compound Library Hematonosis Compound Library Apoptosis Compound Library

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Keywords

SKI-178 1259484-97-3 Apoptosis GPCR/G Protein S1P Receptor resistant SphK cytotoxic myeloid Inhibitor SKI178 leukemia multi-drug inhibit cancer Sphingosine kinase drug sensitive cell SKI 178 inhibitor

 

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