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SphK-I2

  Cat. No.:  DC7295   Featured
Chemical Structure
312636-16-1
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More than 5000 active chemicals with high quality for research!
Field of application
SKI II is a highly selective and non ATP-competitive S1P receptor inhibitor with IC50 of 0.5 μM, while exhibits no inhibitory on other kinases including PI3K, PKCα and ERK2.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 312636-16-1
Synonyms: Sphingosine Kinase Inhibitor;Sphingosine Kinase Inhibitor 2;SKI II (SphK-I2);SphK-I2;SKI II (Sphingosine Kinase Inhibitor)
SMILES: C1=CC(=CC=C1C2=CSC(=N2)NC3=CC=C(C=C3)O)Cl
Formula: C15H11ClN2Os
M.Wt: 302.78
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: SKI-II is a synthetic inhibitor of sphingosine kinase (SK) activity with IC50 of 78 μM for SK1 and 45 μM for SK2.
Target: IC50 value: 78/45 μM (SK1/2) [2] Target: SK
In Vivo: SKI-II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation. In the present study, SKI-II was administered 3-weekly i.p. to LDL-R-/- mice for 16 weeks at a dose previously demonstrated to reduce tumor growth in mice. Preliminary experiments revealed that a single administration of SKI-II produces a significant reduction of plasma S1P with the maximum (40%) observed 12 h after injection. [2]
In Vitro: SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II also reduces the expression of c-Myc and cyclin D1, the downstream target genes of the Wnt signaling pathway. 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 inhibits the proliferation of HepG2 cells by blocking the Wnt/β-catenin signaling pathway. [1]
References: [1]. Liu H, et al. SphK1 inhibitor SKI II inhibits the proliferation of human hepatoma HepG2 cells via the Wnt5A/β-catenin signaling pathway. Life Sci. 2016 Apr 15;151:23-9. [2]. Potì F, et al. SKI-II--a sphingosine kinase 1 inhibitor--exacerbates atherosclerosis in low-density lipoprotein receptor-deficient (LDL-R-/-) mice on high cholesterol diet. Atherosclerosis. 2015 May;240(1):212-5. [3]. Liu Y, et al. SKI-II reverses the chemoresistance of SGC7901/DDP gastric cancer cells. Oncol Lett. 2014 Jul;8(1):367-373.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC10079 CYM5541 CYM5541 is a selective sphingosine-1-phosphate receptor 3 (S1P3) allosteric agonist (EC50 = 72-132 nM).
DC7295 SphK-I2 SKI II is a highly selective and non ATP-competitive S1P receptor inhibitor with IC50 of 0.5 μM, while exhibits no inhibitory on other kinases including PI3K, PKCα and ERK2.
DC9742 Ponesimod Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.
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DC10630 ONO-7300243 ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM.
DC7179 Ki16425 Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively, shows no activity at LPA4, LPA5, LPA6.
DC8889 Ki16198 Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6.
DC10040 Etrasimod(APD334) Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1(S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
DC8088 CYM5442 CYM-5442 is a highly-selective S1P1 (Spingosine 1-Phosphate Receptor 1) agonist.
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