SphK
Sphingosine kinase
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
All Product Categories
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SphK Related Products (62)
Related Products (62)
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Antibodies (1)
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SphK Isoform Comparison
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Phorbol 12-myristate 13-acetate
0 ImagesSynonyms: PMA; TPA; Phorbol myristate acetatePhorbol 12-myristate 13-acetate (PMA; TPA; Phorbol myristate acetate), 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 (Validated by MedChemExpress).
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PF-543
0 ImagesSynonyms: Sphingosine Kinase 1 Inhibitor IIPF-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.
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SKI II
0 ImagesSKI-II is an orally active dual-target inhibitor of SphK1/2 and DES1, with Ki values of 16 µM and 0.3 µM against SphK1 and DES1, respectively. SKI-II activates the PERK-Nrf2 antioxidant pathway by stabilizing Nrf2, and synergizes with Temozolomide (HY-17364) to induce oxidative/endoplasmic reticulum stress and cancer cell death under hypoxic conditions. In vivo, SKI-II inhibits SphK activity, promotes ceramide accumulation and apoptosis, and synergizes with Cisplatin (HY-17394) to reverse drug resistance via the ras/MAPK pathway. SKI-II reduces measles virus replication by inhibiting mTORC1 activity. SKI-II binds to VCP to induce M1 polarization, enhances host tolerance to Staphylococcus aureus infection, and exerts radioprotective effects through Nrf2 activation and accelerated DNA repair. SKI-II can be used in research related to glioblastoma, acute myeloid leukemia, gastric cancer, measles virus infection, Staphylococcus aureus infection, and acute radiation syndrome.
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PF-543 Citrate
0 ImagesSynonyms: Sphingosine Kinase 1 Inhibitor II CitratePF-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.
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Opaganib
0 ImagesSynonyms: ABC294640Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.
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N,N-Dimethylsphingosine
0 ImagesN,N-Dimethylsphingosine is a sphingosine kinase inhibitor. N,N-Dimethylsphingosine binds competitively to sphingosine kinase and blocks the conversion of sphingosine to sphingosine-1-phosphate. N,N-Dimethylsphingosine inhibits sphingosine-1-phosphate release and aggregation of platelets, and also exerts pro-apoptotic effects by resetting ceramide/sphingosine-1-phosphate homeostasis. N,N-Dimethylsphingosine can be used in cancer-related research.
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Peretinoin (Standard)
0 ImagesSynonyms: NIK333 (Standard)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].
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Peretinoin
0 ImagesSynonyms: NIK333Peretinoin 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.
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Phorbol 12-myristate 13-acetate (Standard)
0 ImagesCat. No.: HY-18739RCAS No.: 16561-29-8Synonyms: PMA (Standard); TPA (Standard); Phorbol myristate acetate (Standard)Phorbol 12-myristate 13-acetate (PMA; TPA; Phorbol myristate acetate) (Standard) is the analytical standard of Phorbol 12-myristate 13-acetate. This product is intended for research and analytical applications.
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SKI-178
0 ImagesSKI-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.
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SKI-349
0 ImagesSKI-349 is a dual-targeted inhibitor of sphingosine kinase 1/2 (SPHK1/2) and microtubule assembly (MDA). SKI-349 has anticancer activity. SKI-349 can inhibit the vitality, invasion, and AKT/mTOR signaling pathway of liver cells.
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SKI V
0 ImagesSKI 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.
