SKI-II


Catalog No. size PriceQuantity
M6940-2 2mg solid $127
M6940-10 10mg solid $516

Description

Cas:312636-16-1

Product Information:

SKI-II is a selective non-lipid inhibitor of sphingosine kinase (IC50 = 0.5 μM). nhibits acute myelogenous leukemia cell growth in vitro and in vivo. SKI-II was more efficient than two known SphK1 inhibitors SK1-I and FTY720 in inhibiting AML cells. Meanwhile, it induced dramatic apoptosis in above AML cells, and the cytotoxicity by SKI-II was almost reversed by the general caspase inhibitor z-VAD-fmk. SKI-II treatment inhibited SphK1 activation, and concomitantly increased level of sphingosine-1-phosphate (S1P) precursor ceramide in AML cells.

 

Chemical Formula: C15H11ClN2OS

 

Exact Mass: 302.0281

 

Molecular Weight: 302.776

 

Elemental Analysis: C, 59.50; H, 3.66; Cl, 11.71; N, 9.25; O, 5.28; S, 10.59

 

Chemical Name:

4-[[4-(4-Chlorophenyl)-2-thiazolyl]amino]phenol

 

InChi Key: 

ZFGXZJKLOFCECI-UHFFFAOYSA-N

 

InChi Code:

InChI=1S/C15H11ClN2OS/c16-11-3-1-10(2-4-11)14-9-20-15(18-14)17-12-5-7-13(19)8-6-12/h1-9,19H,(H,17,18)

 

Smiles Code:

OC1=CC=C(NC2=NC(C3=CC=C(Cl)C=C3)=CS2)C=C1

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro:

SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II promotes the degradation of β-catenin by enhancing Wnt5A.

SKI II (1.25 μM, 48 h) in combination with DDP has a clear synergistic effect in human gastric carcinoma SGC7901/DDP cell line.

 

In Vitro:

Chronic SKI II (50.0 mg/kg, 3-weekly i.p. for 16 weeks) administration leads to permanent reduction of S1P concentrations in plasma in mice.

SKI II (50.0 mg/kg, IP; 100 mg/kg, PO) treatment reduces tumor growth in mice bearing solid tumor model.

 

 

References:

  1. Aurelio L, Scullino CV, Pitman MR, Sexton A, Oliver V, Davies L, Rebello RJ, Furic L, Creek DJ, Pitson SM, Flynn BL. From Sphingosine Kinase to Dihydroceramide Desaturase: A Structure-Activity Relationship (SAR) Study of the Enzyme Inhibitory and Anticancer Activity of 4-((4-(4-Chlorophenyl)thiazol-2-yl)amino)phenol (SKI-II). J Med Chem. 2016 Feb 3. [Epub ahead of print] PubMed PMID: 26780304.

 

  1. Yang L, Weng W, Sun ZX, Fu XJ, Ma J, Zhuang WF. SphK1 inhibitor II (SKI-II) inhibits acute myelogenous leukemia cell growth in vitro and in vivo. Biochem Biophys Res Commun. 2015 May 15;460(4):903-8. doi: 10.1016/j.bbrc.2015.03.114. Epub 2015 Mar 28. PubMed PMID: 25824043.

 

  1. Potì F, Ceglarek U, Burkhardt R, Simoni M, Nofer JR. SKI-II--a sphingosine kinase 1 inhibitor--exacerbates atherosclerosis in low-density lipoprotein receptor-deficient (LDL-R-/-) mice on high cholesterol diet. Atherosclerosis. 2015 May;240(1):212-5. doi: 10.1016/j.atherosclerosis.2015.03.020. Epub 2015 Mar 16. PubMed PMID: 25801013.

 

  1. Li PH, Wu JX, Zheng JN, Pei DS. A sphingosine kinase-1 inhibitor, SKI-II, induces growth inhibition and apoptosis in human gastric cancer cells. Asian Pac J Cancer Prev. 2014;15(23):10381-5. PubMed PMID: 25556479.

 

  1. Liu Y, Zhu Z, Cai H, Liu Q, Zhou H, Zhu Z. SKI-II reverses the chemoresistance of SGC7901/DDP gastric cancer cells. Oncol Lett. 2014 Jul;8(1):367-373. Epub 2014 Apr 25. PubMed PMID: 24959278; PubMed Central PMCID: PMC4063656.

 

Products are for research use only. Not for human use.

 

 

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