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SKI II

SKU: orb1222379

Description

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.
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Images & Validation

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SKI II

Key Properties

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CAS Number312636-16-1
MW302.78
Purity>98% (HPLC)
FormulaC15H11ClN2OS
SMILESc1cc(ccc1c1csc(n1)Nc1ccc(cc1)O)Cl
TargetSphK1
SolubilityDMSO : ≥ 100 mg/mL; 330.27 mM

Bioactivity

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In Vivo
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. Animal model: 8 week-old female LDL-R-/-mice. Dosage: 50.0 mg/kg. Administration: IP injection daily, 3 days a week for 16 weeks. Result: A single administration of produced a significant reduction of plasma S1P with the maximum (~40%) observed 12 h after injection. At sacrifice (72 h after last injection) S1P levels were 266 ± 18 ng/mL and 328 ± 30 ng/mL in the SKI-II-treated and control groups, respectively. Animal model: BALB/c mouse solid tumor model that uses JC mammary adenocarcinoma cells. Dosage: 50.0 mg/kg. Administration: IP injection daily, 3 days a week for 16 weeks. Result: Had strong inhibition of tumor growth from the start of treatment of 65%, with no toxicity or weight loss. Animal model: BALB/c JC tumor model. Dosage: 100 mg/kg. Administration: PO every other day. Result: Caused significant antitumor activity in well-established tumors as early as day 5, with maximal response seen at the end of the study. Showed 79% inhibition of tumor growth from the start of treatment.
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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. Cell Cytotoxicity Assay Cell line: The human gastric carcinoma SGC7901/DDP cell line. Concentration: 0 μM, 1.25 μM (combined with DDP). Incubation time: 48 hours. Result: SKI II in combination with DDP had a greater effect on the SGC-7901/DDP cells compared with DDP or SKI II alone.
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Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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SKI-II | SKI II. Sphingosine kinase inhibitor II

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  • SKI II

    SKI II [orb1300568]

    99.97%

    312636-16-1

    302.78

    C15H11ClN2OS

    10 mg, 200 mg, 25 mg, 50 mg, 100 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Quick Database Links

Gene Symbol
SphK1

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SKI II (orb1222379)

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