2. Signaling Pathways
  3. Immunology/Inflammation
  4. SphK

SphK

Sphingosine kinase

SphK

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Sphingosine kinase (SphK1 and SphK2) is a lipid enzyme that catalyses the phosphorylation of sphingosine to form sphingosine 1-phosphate (S1P). Two isoforms of SphK are found in mammalian organisms, SphK1 and SphK2. SphK1 is found primarily in the cytoplasm and the plasma membrane of erythrocyte, endothelial and mast cells. SphK2 is larger and localized to the endoplasmic reticulum, nucleus, and mitochondria.

S1P binds to five different plasma membrane sphingosine 1-phosphate receptors (S1P1-5) and can regulate intracellular target proteins. S1P has a wide range of biological functions including promotion of cellular proliferation and survival, immune cell trafficking, stimulation of angiogenesis, and regulation of vascular integrity. Accumulation of S1P has been linked to the development/progression of cancer and various other diseases including, but not limited to, asthma, inflammatory bowel disease, rheumatoid arthritis, and diabetic nephropathy. Thus, the biosynthetic route to S1P is a logical target for drug discovery. SphK1 and SphK2 isozymes are also recognized therapeutic targets.

SphK Isoform Specific Products:

SphK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-106029
    4α-TPA
    		Control ≥99.0%
    4α-TPA is an inactive form of TPA, and is used as a negative control for TPA-activated events.
    4α-TPA
  • HY-150513
    SLP9101555
    		Inhibitor 99.40%
    SLP9101555 (compound 14c) is a potent and selective SphK2 (sphingosine kinase 2) inhibitor (Ki=90 nM) with 200-fold selectivity over SphK1. SLP9101555 markedly decreases extracellular S1P (sphingosine 1-phosphate) levels.
    SLP9101555
  • HY-12895
    SKI V
    		Inhibitor 98.95%
    SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC50 of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC50 of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity.
    SKI V
  • HY-15779
    K145
    		Inhibitor
    K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity.
    K145
  • HY-15425B
    PF-543 hydrochloride
    		Inhibitor
    PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.
    PF-543 hydrochloride
  • HY-150615
    SphK1-IN-2
    		Inhibitor
    SphK1-IN-2 is a potent, selective SphK1 inhibitor with IC50 values of 19.81 nM and ＞10 μM for SphK1 and SphK2, respectively. SphK1-IN-2 exhibits anti-proliferative activities and induces cell cycle arrest and apoptosis. SphK1-IN-2 can be used for cancer research.
    SphK1-IN-2
  • HY-151350
    SphK2-IN-1
    		Inhibitor
    SphK2-IN-1 is a SphK2 inhibitor (IC50: 0.359 μM). SphK2-IN-1 can be used in the research of cancer, inflammation, neurological and cardiovascular disorders.
    SphK2-IN-1
  • HY-RS13667
    SPHK2 Human Pre-designed siRNA Set A
    		Inhibitor

    SPHK2 Human Pre-designed siRNA Set A contains three designed siRNAs for SPHK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SPHK2 Human Pre-designed siRNA Set A
    SPHK2 Human Pre-designed siRNA Set A
  • HY-117563
    CAY10621
    		Inhibitor
    CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research.
    CAY10621
  • HY-143296
    SphK1-IN-1
    		Inhibitor
    SphK1-IN-1 (compound 48) is a SphK1 inhibitor with effective antitumor activity. SphK1-IN-1 inhibits SphK1 ATPase with an IC50 value of 4.02 μM. SphK1-IN-1 can be used for the research of cancer.
    SphK1-IN-1
  • HY-120152
    SLP7111228
    		Inhibitor
    SLP7111228 is a SphK1 inhibitor. SLP7111228 reduces LPS-induced TNFα and IL-1β production. SLP7111228 can be used in neuroinflammatory diseases research.
    SLP7111228
  • HY-124863A
    (R)-AAL
    		Substrate
    (R)-AAL is an immunomodulator. (R)-AAL decreases circulating T lymphocytes in rats, with an ID50 value of 0.009 mg/kg. (R)-AAL is a substrate of sphingosine kinase (SphK), which catalyzes the phosphorylation of (R)-AAL.
    (R)-AAL
  • HY-RS13666
    Sphk1 Rat Pre-designed siRNA Set A
    		Inhibitor

    Sphk1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sphk1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sphk1 Rat Pre-designed siRNA Set A
    Sphk1 Rat Pre-designed siRNA Set A
  • HY-RS13664
    SPHK1 Human Pre-designed siRNA Set A
    		Inhibitor

    SPHK1 Human Pre-designed siRNA Set A contains three designed siRNAs for SPHK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SPHK1 Human Pre-designed siRNA Set A
    SPHK1 Human Pre-designed siRNA Set A
  • HY-RS13668
    Sphk2 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Sphk2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sphk2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sphk2 Mouse Pre-designed siRNA Set A
    Sphk2 Mouse Pre-designed siRNA Set A
  • HY-148262
    SphK1-IN-3
    		Inhibitor
    SphK1-IN-3 is an effective sphingosine kinase-1 (SphK1) inhibitor. SphK1-IN-3 inhibits SphK1 kinase activity with an IC50 value of 2.48 μM. SphK1-IN-3 can be used for the research of many diseases such as cancer, rheumatoid arthritis, diabetes, asthma, and pulmonary fibrosis.
    SphK1-IN-3
  • HY-151351
    SphK2-IN-2
    		Inhibitor
    SphK2-IN-2 (21g) is a potent and selective SphK2 inhibitor with an IC50 value of 0.23 μM.
    SphK2-IN-2
  • HY-RS13665
    Sphk1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Sphk1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sphk1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sphk1 Mouse Pre-designed siRNA Set A
    Sphk1 Mouse Pre-designed siRNA Set A
  • HY-W019781
    Biotinylated sphingosine
    Biotinylated sphingosine (Biotinyl-Sph) is a substrate of sphingosine kinase that can b used to detect the phosphorylation activity of sphingosine kinase 1 (SPHK1) and SPHK2.
    Biotinylated sphingosine
  • HY-120268
    SLM6031434
    		Inhibitor
    SLM6031434 is a highly selective sphingosine kinase 2 (SphK2) inhibitor with Kis of 0.4 μM, 0.5 μM, >20 μM, 22 μM for mSphK2, rSphK2, mSphK1 and rSphK1, respectively. SLM6031434 decrease Sphingosine 1-phosphate (S1P) levels in U937 monocytic leukemia cells. SLM6031434 has the potential for renal fibrosis research.
    SLM6031434
Cat. No. Product Name / Synonyms Application Reactivity
SphK Isoform Comparison

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