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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 <a href="/target/CDK" style="display: inline; color: #c13a36">CDK</a>1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival <a href="/target/BCL" style="display: inline; color: #c13a36">BCL</a>-2 family members, <a href="/target/BCL" style="display: inline; color: #c13a36">BCL</a>-2 and <a href="/target/BCL" style="display: inline; color: #c13a36">BCL</a>-xl, as well as the phosphorylation and subsequent degradation of Mcl-1.

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SKI-178, CAS 1259484-97-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 48.00
5 mg	In stock	$ 70.00
10 mg	In stock	$ 121.00
25 mg	In stock	$ 233.00
50 mg	In stock	$ 380.00
100 mg	In stock	$ 567.00
1 mL * 10 mM (in DMSO)	In stock	$ 80.00

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Purity: 99.2%

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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	394.431
Formula	C21H22N4O4
CAS No.	1259484-97-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 50 mg/mL (126.77 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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 Bioactive Compounds Library Max NO PAINS Compound Library GPCR Compound Library Bioactive Compound Library Hematonosis Compound Library Anti-Cancer Compound Library Apoptosis Compound Library Kinase Inhibitor Library

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Keywords

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

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