SK1-I

BML-EI411

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Sphingosine kinase 1 inhibitor exclusive to Enzo Life Sciences

SK1-I is a sphingosine analog and a sphingosine competitive inhibitor specific for sphingosine kinase 1 (SK1), with k_i~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.

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Product Details

Alternative Name	(2R,3S,4E)-N-methyl-5-(4′-pentylphenyl)-2-aminopent-4-ene-1,3-diol . HCl
Appearance	White solid.
CAS	1072443-89-0
Couple Target	Sphingosine kinase
Couple Type	Inhibitor
Formula	C₁₇H₂₇NO₂. HCl
Identity	Determined by NMR.
MW	313.9
Purity	≥98% (HPLC)
Solubility	Soluble in water or DMSO (100 mM).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored at -20°C.
Handling	Protect from light and air.
Long Term Storage	-20°C
Shipping	Dry Ice

Regulatory Status	RUO – Research Use Only

Regulatory role of SphK1 in TLR7/9-dependent type I interferon response and autoimmunity: S. Mohammed, et al.; FASEB J. 34, 4329 (2020), Abstract — Full Text
Sphingosine-1-phosphate signaling modulates terminal erythroid differentiation through the regulation of mitophagy: Yang, C., Hashimoto, M., et al.; Exp. Hematol. 72, 47 (2019), Abstract
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
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
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
Sphingosine Kinases Signalling in Carcinogenesis: G. Marfe, et al.; Mini Rev. Med. Chem. 15, 300 (2015), Application(s): Inhibition of Sphingosine kinase 1, Abstract
Identification of SPHK1 as a therapeutic target and marker of poor prognosis in cholangiocarcinoma: Chen, M. H., Yen, C. C., et al.; Oncotarget 6, 23594 (2015), 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

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SK1-I

BML-EI411

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