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Sphingosine kinase 1 inhibitor exclusive to Enzo Life Sciences
BML-EI411-0025 25 mg Inquire for pricing
BML-EI411-0005 5 mg Inquire for pricing
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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 Specification

Alternative Name:(2R,3S,4E)-N-methyl-5-(4'-pentylphenyl)-2-aminopent-4-ene-1,3-diol . HCl
Formula:C17H27NO2 . HCl
Purity:≥98% (HPLC)
Identity:Determined by NMR.
Appearance:White solid.
Solubility:Soluble in water or DMSO (100 mM).
Shipping:Shipped on Dry Ice
Long Term Storage:-20°C
Use/Stability:Stable for at least 1 year after receipt when stored at -20°C.
Handling:Protect from light and air.
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Product Literature References

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; Full Text
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; Full Text
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; Full Text
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; Full Text

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