For research use only.

Catalog No.S7176 Synonyms: SphK-I2

12 publications

SKI II Chemical Structure

CAS No. 312636-16-1

SKI II (SphK-I2) is a highly selective and non ATP-competitive sphingosine kinase (SphK) inhibitor with IC50 of 0.5 μM, while exhibiting no inhibitory action on other kinases including PI3K, PKCα and ERK2.

Selleck's SKI II has been cited by 12 publications

5 Customer Reviews

  • Transwell migration and invasion assays were performed. The stained cells were counted in five random fields at ×200 magnification, and the average number was taken. The average number of Control group (cells transduced with pLVX and treated with DMSO) was set as 100%, and relative migration and invasion of other groups was calculated by comparison of the cell number with the average number of control group. ***P < 0.001 versus pLVX + DMSO; ###P < 0.001 versus pLVX-p53 + DMSO.

    Cancer Cell Int, 2018, 18:202. SKI II purchased from Selleck.

    Inhibition of sphingosine kinase 1 in cell-free extract and in vitro. a 1 µM of compounds SK-A to SK-F and SKI-II (commercial inhibitor of SK used as a positive control) were incubated in the presence of recombinant SK1 extract (in excess), 1 µM of ATP, and 1 µM exogenous sphingosine for 1 h. b MDA-MB-231 cells were incubated with 1 µM of compounds SK-A to SK-F and SKI-II for 6 h. SK1 activity was measured as described in materials and methods. Columns, means of three independent experiments normalised to vehicle; bars, SEM. (ns, non-significant; *p < 0.05; **p < 0.01).

    Breast Cancer Res Treat, 2018, 172(1):33-43. SKI II purchased from Selleck.

  • D, representative merged IF images with DAPI nuclei staining (blue) in untreated (“Ctl”) and CoCl2-treated cells without (“Veh”), and with SKI-II co-treatment. Scale bar = 30 μm. N=5 independent samples per group. oligodendrocytes(defined by MBP immunoreactivity, red), oligodendrocyte progenitor cell(defined by NG2 immunoreactivity, green).

    Neurochemistry International, 2016, 94: 90-97.. SKI II purchased from Selleck.

    C are representative Klüver-Barrera staining for N = 3 per group, scale bars = 120 μm. Panels on the right showing magnification of the areas defined by the black squares on the left panels, scale bars = 30 μm. D, representative immunoblot and E, bar graph of white matter tissue myelin basic protein (MBP) immunoreactivity (as mean ± S.E.M. fold-change relative to mean value of sham operated, N = 6 per group). One-way ANOVA, F(2, 15) = 9.7, *p < 0.05 with post-hoc Bonferroni correction.

    Neurochem Int, 2016, 94:90-7. SKI II purchased from Selleck.

  • Protein expression of sphingosine kinase 1 (SphK1), FAK, p-FAK, Slug, vimentin, N-cadherin, E-cadherin in Caco2, HT29, RKO, HCT116 cells. '−' indicates culture without SKI-II or PF-562271, while '+' indicates treatment with SKI-II 20 µM for 48h or PF-562271 5 µM for 48 h.

    Int J Mol Med, 2017, 39(5):1277-1284. SKI II purchased from Selleck.

Purity & Quality Control

Choose Selective SPHK Inhibitors

Biological Activity

Description SKI II (SphK-I2) is a highly selective and non ATP-competitive sphingosine kinase (SphK) inhibitor with IC50 of 0.5 μM, while exhibiting no inhibitory action on other kinases including PI3K, PKCα and ERK2.
Sphingosine Kinase [1]
0.5 μM
In vitro

SKI II potently inhibits endogenous SK activities in the breast cancer cell line MDA-MB-231. SKI II demonstrates significantly antiproliferative effects in human cancer cell lines including T-24, MCF-7, MCF-7/VP, NCI/ADR with IC50 of 4.6 μM , 1.2 μM, 0.9 μM and 1.3 μM, respectively. SKI II also induces apoptosis of T24 cells consistent with the hypothesized consequence of reducing S1P levels. [1] As demonstrated previously in MDA-MB-231 cells, SKI II decreases S1P formation in JC cells in a concentration-dependent manner, with IC50 of 12 μM. [2] In addition, SKI-II can reverse drug resistance of SGC7901/DDP to cisplatin by down-regulating expression of P-gp and up-regulating apoptosis through down-regulation of SphK1. [3]

In vivo SKI II (50 mg/kg) after intraperitoneal or oral administration significantly decreases tumor growth a syngeneic Balb/c mouse solid tumor model that uses JC mammary adenocarcinoma cells relative to control groups with no overt toxicity or weight loss.[2] SKI-II (50 mg/kg ip) ameliorates antigen-induced bronchial smooth muscle hyperresponsiveness in mice by endogenously inhibiting generation of S1P. [4]


Kinase Assay:[1]
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SK Assay:

A medium-throughput assay suitable for screening for inhibitors of recombinant human SK has been established. Briefly, 5 μg of purified GST-SK fusion protein are combined with 12 nM sphingosine, which contains a 100-fold dilution of [3-3H]sphingosine (20 Ci/mmol), 1 mM ATP, 1 mM magnesium chloride, and 200 μL of assay buffer [20 mM Tris HCl (pH 7.4), 20% glycerol, 1 mM beta-mercaptoethanol, 1 mM EDTA, 20 mM zinc chloride, 1 mM sodium orthovanadate, 15 mM sodium fluoride, and 0.5 mM 4-deoxypyridoxine]. Assays are run for 30 min at 25°C with shaking and contains either 1% DMSO or 5 g/mL test compound, which corresponds to concentrations of 10–25 μM. The reactions are terminated with 50 μL of concentrated ammonium hydroxide, followed by extraction of the assay mixture with chloroform:methanol (2:1). The aqueous portion is transferred to scintillation vials and radioactivity is quantified as a measure of [3H]]S1P formation using a Beckman LS 3801 Scintillation Counter. The intra-assay coefficient of variation is ~10%, whereas interassay variation is ~20%.
Cell Research:[1]
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  • Cell lines: T-24, MCF-7, MCF-7/VP, NCI/ADR cell lines
  • Concentrations: ~50 μM
  • Incubation Time: 48 hours
  • Method: T24, MCF-7, MCF-7/VP, and NCI/ADR cells are plated into 96-well tissue culture plates at ~15% confluency. After 24 hours, cells are treated with various concentrations of inhibitors. After an additional 48 hours, cell survival is assayed using the sulforhodamine B assay.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: JC xenografts are established in mice
  • Dosages: ~100 mg/kg
  • Administration: Intraperitoneal administration or oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 61 mg/mL (201.46 mM)
Water Insoluble
Ethanol '61 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 302.78


CAS No. 312636-16-1
Storage powder
in solvent
Synonyms SphK-I2
Smiles C1=CC(=CC=C1C2=CSC(=N2)NC3=CC=C(C=C3)O)Cl

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID