SK1-I is a sphingosine analog and a sphingosine competitive inhibitor specific for sphingosine kinase 1 (SK1), with ki~10µM and excellent water solubility. It is not to be confused with SKI-I, 5-naphthalen-2-yl-2H-pyrazole-3-carboxylic acid (2-hydroxy-naphthalen-1-ylmethylene)-hydrazide, CAS 306301-68-8, a noncompetitive inhibitor of both SK1 and SK2 with poor water solubility (K.J. French, et al., 2006; N.J. Pyne and S. Pyne, 2010). SK1-I does not inhibit SK2, PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. Not only does it decrease sphingosine-1-phosphate levels, it also causes an accumulation of its proapoptotic precursor ceremide. Inhibits tumor cell growth in vitro and in vivo.
Product Details
| Alternative Name: | (2R,3S,4E)-N-methyl-5-(4'-pentylphenyl)-2-aminopent-4-ene-1,3-diol . HCl |
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| Formula: | C17H27NO2 . HCl |
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| MW: | 313.9 |
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| CAS: | 1072443-89-0 |
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| Purity: | ≥98% (HPLC) |
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| Identity: | Determined by NMR. |
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| Appearance: | White solid. |
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| Solubility: | Soluble in water or DMSO (100 mM). |
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| Shipping: | Dry Ice |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stable for at least 1 year after receipt when stored at -20°C. |
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| Handling: | Protect from light and air. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Regulatory role of SphK1 in TLR7/9-dependent type I interferon response and autoimmunity: S. Mohammed, et al.; FASEB J.
34, 4329 (2020),
Abstract;
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Sphingosine kinase 1 activation by estrogen receptor α36 contributes to tamoxifen resistance in breast cancer: M.A. Maczis, et al.; J. Lipid Res.
59, 2297 (2018),
Abstract;
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TP53 is required for BECN1- and ATG5-dependent cell death induced by sphingosine kinase 1 inhibition: S. Lima, et al.; Autophagy
11, 1 (2018),
Abstract;
A novel E2F/Sphingosine kinase 1 axis regulates anthracycline response in squamous cell carcinoma: M. Hazar-Rethinam, et al.; Clin. Cancer Res.
21, 417 (2015),
Application(s): Inhibition of Sphingosine kinase 1 in doxorubicin-treated SCC cells and in vivo.,
Abstract;
Inhibition of Sphingosine Kinase 1 Ameliorates Angiotensin II-induced Hypertension and Inhibits Transmembrane Calcium Entry via Store-Operated Calcium Channel: P. C. Wilson, et al.; Mol. Endocrinol.
29, 896 (2015),
Application(s): Cell Culture,
Abstract;
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Sphingosine Kinases Signalling in Carcinogenesis: G. Marfe, et al.; Mini Rev. Med. Chem.
15, 300 (2015),
Application(s): Inhibition of Sphingosine kinase 1,
Abstract;
K63-linked polyubiquitination of transcription factor IRF1 is essential for IL-1-induced production of chemokines CXCL10 and CCL5.: K. B. Harikumar, et al.; Nat. Immunol.
15, 231 (2014),
Application(s): Inhibition of Sphingosine kinase 1 in primary human astrocytes and mice,
Abstract;
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LRIG1 modulates aggressiveness of head and neck cancers by regulating EGFR-MAPK-SPHK1 signaling and extracellular matrix remodeling: J. J. C. Sheu, et al.; Oncogene
33, 1375 (2014),
Application(s): Inhibition of Sphingosine kinase 1 in head and neck cancer TW06 cells,
Abstract;
Role of sphingosine kinase 1 and sphingosine-1-phosphate in CD40 signaling and IgE class switching: E. Y. Kim, et al.; FASEB J.
28, 4347 (2014),
Application(s): Inhibition of Sphingosine kinase 1 in human tonsil B cells, mouse splenic B cells and in mice,
Abstract;
Sphingosine kinase-1 enhances resistance to apoptosis through activation of PI3K/Akt/NF-κB pathway in human non–small cell lung cancer: L. Song et al.; Clin. Cancer Res.
17, 1839 (2011),
Abstract;
Targeting sphingosine kinase 1 inhibits Akt signaling, induces apoptosis, and suppresses growth of human glioblastoma cells and xenografts: D. Kapitonov et al.; Cancer Res.
69, 6915 (2009),
Abstract;
A selective sphingosine kinase 1 inhibitor integrates multiple molecular therapeutic targets in human leukemia: S.W. Paugh et al.; Blood
112, 1382 (2008),
Abstract;
General Literature References
Sphingosine-1-phosphate and cancer: N.J. Pyne & S. Pyne; Nat. Rev. Cancer
10, 489 (2010),
Abstract;
Antitumor Activity of Sphingosine Kinase Inhibitors: K.J. French, et al.; J. Pharmacol. Exp. Ther.
318, 596 (2006),
Abstract;
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