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-18739
    Phorbol 12-myristate 13-acetate
    		Activator 99.80%
    Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator. Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells.
    Phorbol 12-myristate 13-acetate
  • HY-15425
    PF-543
    		Inhibitor 99.85%
    PF-543 (Sphingosine Kinase 1 Inhibitor II) 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 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy.
    PF-543
  • HY-15425A
    PF-543 Citrate
    		Inhibitor 99.47%
    PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) 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 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy.
    PF-543 Citrate
  • HY-13822
    SKI II
    		Inhibitor 99.78%
    SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation.
    SKI II
  • HY-16015
    Opaganib
    		Inhibitor 99.94%
    Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.
    Opaganib
  • 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
  • HY-16015A
    Opaganib hydrochloride
    		Inhibitor
    Opaganib (ABC294640) hydrochloride is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.
    Opaganib hydrochloride
  • HY-12900
    RB-005
    		Inhibitor
    RB-005 is a selective inhibitor of sphingosine kinase 1 (SK1) (IC50=3.6 µM), with weaker inhibition of another isoenzyme, SK2. The selective inhibition of RB-005 helps to distinguish the biological functions and roles of SK1 and SK2, which can be used in the study of inflammatory diseases and cancer.
    RB-005
  • HY-15779A
    K145 hydrochloride
    		Inhibitor 99.88%
    K145 hydrochloride 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 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.
    K145 hydrochloride
  • HY-100008
    Peretinoin
    		Inhibitor 99.79%
    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. 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. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM.
    Peretinoin
  • HY-124042
    K6PC-5
    		Activator 99.85%
    K6PC-5, a ceramide derivative, is a sphingosine kinase 1(SPHK1) activator and elicites a rapid transient increase in intracellular calcium levels. K6PC-5 has the potential for skin diseases involving abnormal keratinocyte, and neurodegeneration and virus infection research.
    K6PC-5
  • HY-12892
    SKI-178
    		Inhibitor 98.91%
    SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.
    SKI-178
  • HY-101572
    MHP
    		Activator 98.23%
    MHP (Methyl caprooyl tyrosinate) is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production. MHP (Methyl caprooyl tyrosinate) enhances antimicrobial defense and innate immunity.
    MHP
  • HY-19794
    MP-A08
    		Inhibitor ≥98.0%
    MP-A08 is a highly selective ATP competitive sphingosine kinase (SPHK1) inhibitor that targets both SphK1 and SphK2 with Ki values of 6.9 ± 0.8 μM and 27 ± 3 μM, respectively.
    MP-A08
  • HY-108491
    N,N-Dimethylsphingosine
    		Inhibitor ≥99.0%
    N,N-Dimethylsphingosine is a potent inhbitor of SphK (sphingosine kinase) as an endogenous metabolite of sphingosine produced in various tissues and tumor cell lines.
    N,N-Dimethylsphingosine
  • HY-119016
    SK1-I
    		Inhibitor 98.47%
    SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity.
    SK1-I
  • HY-115735
    SKI-I
    		Inhibitor 99.14%
    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-101805
    SK1-IN-1
    		Inhibitor 98.72%
    SK1-IN-1 is a potent sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 58 nM.
    SK1-IN-1
  • HY-147282
    Amgen-23
    		Inhibitor 99.00%
    Amgen-23 (compound 23) is a potent sphingosine kinases (SPHK) inhibitor with IC50 values of 20 nM and 1.6 μM for SPHK1 and SPHK2, respectively. Amgen-23 can be used for researching anticancer.
    Amgen-23
  • HY-119016A
    SK1-​I hydrochloride
    		Inhibitor 99.49%
    SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity.
    SK1-​I hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
SphK Isoform Comparison

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