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-115735
    SKI-I
    		Inhibitor 99.73%
    SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines.
    SKI-I
  • 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-120268A
    SLM6031434 hydrochloride
    		Inhibitor 99.1%
    SLM6031434 hydrochloride is the hydrochloride salt form of SLM6031434 (HY-120268). SLM6031434 is a highly selective sphingosine kinase 2 (SphK2) inhibitor with an IC50 value of 0.4 μM for SphK2. SLM6031434 exerts anti-fibrotic effects by increasing sphingosine accumulation and Smad7 expression. SLM6031434 demonstrates effective anti-fibrotic efficacy in a unilateral ureteral obstruction (UUO)-induced tubulointerstitial fibrosis mouse model. SLM6031434 can be used for the study of proteinuric kidney diseases or chronic kidney disease (CKD).
    SLM6031434 hydrochloride
  • HY-148707
    SphK1&2-IN-1
    		Inhibitor 98.47%
    SphK1&2-IN-1 is a SphK inhibitor targeting to SphK1 and SphK2. SphK1&2-IN-1 has thermal stability.
    SphK1&2-IN-1
  • HY-150513
    SLP9101555
    		Inhibitor 99.82%
    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-124863A
    (R)-AAL
    		Substrate 99.90%
    (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-151350
    SphK2-IN-1
    		Inhibitor 99.61%
    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-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-117563
    CAY10621
    		Inhibitor 99.3%
    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-151351
    SphK2-IN-2
    		Inhibitor 99.35%
    SphK2-IN-2 (21g) is a potent and selective SphK2 inhibitor with an IC50 value of 0.23 μM.
    SphK2-IN-2
  • 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-120152A
    SLP7111228 hydrochloride
    		Inhibitor 98.01%
    SLP7111228 hydrochloride is a selective sphingosine kinase 1 (SphK1) inhibitor and anti-inflammatory agent. SLP7111228 hydrochloride selectively inhibits SphK1 and reduces the production of sphingosine-1-phosphate. SLP7111228 hydrochloride decreases lipopolysaccharide-induced TNFα and IL-1β levels. SLP7111228 hydrochloride alleviates obliterative pulmonary arteriopathy, increases cardiac index and decreases total pulmonary vascular resistance index. SLP7111228 hydrochloride can be used in research related to neuroinflammatory diseases and pulmonary hypertension.
    SLP7111228 hydrochloride
  • HY-100008R
    Peretinoin (Standard)
    		Inhibitor
    Peretinoin (Standard) is the analytical standard of Peretinoin. This product is intended for research and analytical applications. Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1[1]. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression[2]. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM[3].
    Peretinoin (Standard)
  • 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-16621
    PPI-4955
    		Agonist
    PPI-4955 is a subtype 1 (S1P₁) agonist of sphingosine-1-phosphate receptor with an EC50 of 1.62 nM. PPI-4955-P (the active phosphorylated form) exhibits excellent receptor selectivity and affinity, and the IC50 values for hS1P₁, hS1P₃, hS1P₄, and hS1P₅ are 0.23, 2000, 6.5, and 184 nM respectively. PPI-4955 has significantly improved in vivo phosphorylation efficiency, which can reduce lymphocytes and improve cardiovascular risk. PPI-4955 can be used in immunomodulation research.
    PPI-4955
  • HY-120268
    SLM6031434
    		Inhibitor
    SLM6031434 is a highly selective sphingosine kinase 2 (SphK2) inhibitor with an IC50 value of 0.4 μM for SphK2. SLM6031434 exerts anti-fibrotic effects by increasing sphingosine accumulation and Smad7 expression. SLM6031434 demonstrates effective anti-fibrotic efficacy in a unilateral ureteral obstruction (UUO)-induced tubulointerstitial fibrosis mouse model. SLM6031434 can be used for the study of proteinuric kidney diseases or chronic kidney disease (CKD).
    SLM6031434
  • 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
  • HY-178992
    SphK1-IN-4
    		Inhibitor
    SphK1-IN-4 (Compound 6b) is a sphingosine kinase 1 (SphK1) inhibitor. SphK1-IN-4 can be used for the research of cancer, such as lung cancer.
    SphK1-IN-4
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
SphK Isoform Comparison

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