2. Signaling Pathways
  3. Immunology/Inflammation
  4. SphK
  5. SphK1 Isoform

SphK1

Sphingosine kinase 1 (SphK1) is a key rate-limiting enzyme in sphingolipid metabolism that phosphorylates sphingosine to generate sphingosine-1-phosphate (S1P), thereby regulating the sphingolipid rheostat and multiple cellular processes including survival, proliferation, migration, inflammation, and vascular remodeling[1]. S1P produced by SphK1 functions as a bioactive signaling mediator and activates downstream pathways through S1P receptors, contributing to intracellular signaling and cell-environment communication[1][2]. Mechanistically, SphK1 is activated by diverse stimuli, including cytokines, growth factors, and MAPK signaling, and translocates from the cytoplasm to the plasma membrane where its catalytic activity is enhanced[1]. Dysregulated SphK1 expression or activity has been reported in numerous cancers and inflammatory disorders, and elevated SphK1 is frequently associated with tumor progression, drug resistance, and unfavorable clinical outcomes[2][3][4]. In experimental disease models, SphK1-dependent signaling contributes to inflammatory responses, immune-cell regulation, and cancer cell survival, highlighting its importance in both tumor biology and immune-mediated pathology[1][3]. Compared with the related isoform SphK2, SphK1 is primarily linked to cell growth and survival signaling, whereas SphK2 exhibits distinct subcellular localization patterns and is more closely associated with apoptosis regulation and epigenetic functions[1][5]. This functional divergence has stimulated the development of isoform-selective pharmacological tools. For experimental applications, several SphK1 inhibitors, including PF-543, SK1-I, and Safingol, have been widely used to investigate SphK1-dependent signaling and evaluate the therapeutic potential of targeting the SphK1/S1P axis in cancer and inflammatory diseases[1][3].

SphK1 Related Products (25):

Cat. No. Product Name Effect Purity
  • 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.
  • 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.
  • HY-124042
    K6PC-5
    		Activator 99.27%
    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.
  • HY-119016
    SK1-I
    		Inhibitor 98.83%
    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.
  • HY-12892
    SKI-178
    		Inhibitor 99.29%
    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.
  • HY-124368
    RB-042
    		Inhibitor
    RB-042 is a SK1 and SK2 inhibitor with IC50 values of 5.3 μM and 5.0 μM, respectively. RB-042 is applicable to the research of inflammatory diseases.
  • HY-184271
    SphK1-IN-5
    		Inhibitor
    SphK1-IN-5 is an orally active selective inhibitor of sphingosine kinase 1 (SphK1) with an IC50 of 0.87 μM and a Ki of 1.05 μM. SphK1-IN-5 directly binds to the ATP-binding pocket of SphK1 and enhances the thermal stability of this protein. SphK1-IN-5 regulates sphingolipid homeostasis: it increases sphingosine (Sph) levels and decreases sphingosine-1-phosphate (S1P) levels by inhibiting SphK1-mediated conversion of Sph to S1P. SphK1-IN-5 induces apoptosis in MC38 colon cancer cells, causes cell cycle arrest, inhibits cell migration, and exerts broad-spectrum antiproliferative effects against various tumor cells. SphK1-IN-5 exhibits antitumor activity in a mouse colon tumor model. SphK1-IN-5 can be used for research on colon cancer.
  • HY-12896
    SLR080811
    		Inhibitor
    SLR080811 is a guanidine-based selective sphingosine kinase 2 (SphK2) inhibitor with a Ki of 1.3 μM, exhibiting ~10-fold selectivity over SphK1 (Ki = 12 μM). SLR080811 reduces sphingosine 1-phosphate (S1P) levels in vitro, but drives a SphK1-dependent increase in S1P in mice. SLR080811 can be used for cancers and fibrosis research.
  • 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.
  • HY-101572
    MHP
    		Activator 98.57%
    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.
  • HY-101805
    SK1-IN-1
    		Inhibitor 98.10%
    SK1-IN-1 is a potent sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 58 nM.
  • HY-147282
    Amgen-23
    		Inhibitor 98.11%
    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.
  • 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.
  • 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).
  • 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.
  • 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.
  • 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.
  • 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.
  • 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).
  • 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.
Cat. No. Product Name / Synonyms Application Reactivity