A lipid enzyme called sphingosine kinase (SphK1 and SphK2) catalyzes the phosphorylation of sphingosine to create sphingosine 1-phosphate (S1P). Mammalian organisms have two SphK isoforms, SphK1 and SphK2. SphK1 is primarily present in the cytoplasm and plasma membrane of mast, endothelial, and erythrocyte cells. SphK2 is bigger and is concentrated in the mitochondria, endoplasmic reticulum, and nucleus.
Sphingosine 1-phosphate (S1P) can control intracellular target proteins by binding to five different sphingosine 1-phosphate receptors on the plasma membrane (S1P1–5). S1P performs a wide range of biological activities, including promoting cellular survival and proliferation, moving immune cells, promoting angiogenesis, and controlling vascular integrity. Accumulation of S1P has been associated with cancer development/progression as well as a number of other illnesses, such as inflammatory bowel disease, rheumatoid arthritis, asthma, and diabetic nephropathy. As a result, the biosynthetic pathway for S1P is an obvious candidate for drug discovery. The isozymes SphK1 and SphK2 are also acknowledged therapeutic targets.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V74302 | Biotinylated sphingosine (Biotinyl-Sph) | 752987-57-8 | Biotinylated sphingosine (Biotinyl-Sph) is a substrate of sphingosine kinase and may be utilized to detect the phosphorylation activity of sphingosine kinase 1 (SPHK1) and SPHK2. |
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V4033 | Defensamide (MHP) | 1104874-94-3 | Defensamide (formerly known as MHP and methyl caprooyl tyrosinate) isa novel and potent activator of sphingosine kinase(SPHK1), and significantly stimulates CAMP mRNA and protein production in KC. |
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V33277 | K145 | 1309444-75-4 | K145 (K-145) is a novel, potent and selective SphK2 (sphingosine kinase-2) inhibitor with anticancer effects. |
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V5052 | K145 HCl | 1449240-68-9 | K145 is a novel and selective SphK2 (sphingosine kinase-2) inhibitor (IC50 = 4.30 μM) with antitumor activity. |
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V23101 | K6PC-5 | 756875-51-1 | K6PC-5, a ceramide analogue, is a sphingosine kinase 1 (SPHK1) activator that causes a transient and rapid increase in intracellular calcium levels. |
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V25815 | MP-A08 | 219832-49-2 | MP-A08 is a selective ATP-competitive SPHK1 inhibitor. |
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V74303 | SK1-I hydrochloride (BML-258 hydrochloride) | 2366222-05-9 | SK1-I HCl (BML-258 HCl) is an analog of sphingosine and an isozyme-specific competitive inhibitor of SPHK1 with a Ki of 10 µM. |
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V14886 | SKI-178 | 1259484-97-3 | SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor (IC50 = 0.1-1.8 μM) which is a novel therapeutic agent for the treatment of AML, including multidrug-resistant/recurrent AML subtypes. |
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V79679 | SphK1-IN-3 | SphK1-IN-3 is a potent inhibitor of sphingosine kinase-1 (SphK1). | |
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V74305 | SphK2-IN-1 | 2927429-64-7 | SphK2-IN-1 is a SphK2 inhibitor (IC50= 0.359 μM). |
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V74304 | SphK2-IN-2 | 2927429-60-3 | SphK2-IN-2 (21g) is a potent and specific SphK2 inhibitor (antagonist) with IC50 of 0.23 μM. |
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