SphK (sphingosine kinase) is the major source of the bioactive lipid and GPCR (G-protein-coupled receptor) agonist S1P (sphingosine 1-phosphate). S1P promotes cell growth, survival and migration, and is a key regulator of lymphocyte trafficking. Inhibition of S1P signalling has been proposed as a strategy for treatment of inflammatory diseases and cancer. S1P is an extracellular ligand at five cognate GPCRs, S1PRs and a consequential intracellular lipid intermediate that affects diverse cellular processes including migration, growth and survival. S1P regulates function and trafficking of immune cells, induces angiogenesis and regulates endothelial cell functions, promotes survival and migration of cancer cells, and has been implicated as an important mediator in the pathogenesis of cancer and autoimmune and allergic diseases.


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SKI II

SKI-II is a synthetic inhibitor of sphingosine kinase (SK) activity with IC50 of 78 μM for SK1 and 45 μM for SK2.IC50 value: 78/45 μM (SK1/2) [2]Target: SKin vitro: SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II also reduces the expression of c-Myc and cyclin D1, the downstream target genes of the Wnt signaling pathway. SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II promotes the degradation of β-catenin by enhancing Wnt5A. SKI II inhibits the proliferation of HepG2 cells by blocking the Wnt/β-catenin signaling pathway. [1]in vivo: SKI-II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation. In the present study, SKI-II was administered 3-weekly i.p. to LDL-R-/- mice for 16 weeks at a dose previously demonstrated to reduce tumor growth in mice. Preliminary experiments revealed that a single administration of SKI-II produces a significant reduction of plasma S1P with the maximum (40%) observed 12 h after injection. [2]

  • CAS Number: 312636-16-1
  • MF: C15H11ClN2OS
  • MW: 302.779
  • Catalog: SPHK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 507.1±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 260.5±32.9 °C

N,N-Dimethylsphingosine

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[1].

  • CAS Number: 119567-63-4
  • MF: C20H41NO2
  • MW: 327.545
  • Catalog: SPHK
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 447.2±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 186.1±27.4 °C

PF-543 (Citrate)

PF-543 Citrate is a novel cell-permeant inhibitor of SPHK1 with a Ki of 4.3 nM and more than 100-fold selectivity for SPHK1 over SPHK2.

  • CAS Number: 1415562-83-2
  • MF: C33H39NO11S
  • MW: 657.72800
  • Catalog: SPHK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PF-543

PF-543 is a novel cell-permeant inhibitor of SPHK1 with a Ki of 4.3 nM and more than 100-fold selectivity for SPHK1 over SPHK2.

  • CAS Number: 1415562-82-1
  • MF: C27H31NO4S
  • MW: 465.604
  • Catalog: SPHK
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 666.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 356.6±31.5 °C

CAY10621(SKI 5C)

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[1].

  • CAS Number: 120005-55-2
  • MF: C26H45NO4
  • MW: 435.640
  • Catalog: SPHK
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 519.0±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 267.7±32.9 °C

SLM 6031434 hydrochloride

SLM6031434 hydrochloride 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 hydrochloride decrease Sphingosine 1-phosphate (S1P) levels in U937 monocytic leukemia cells. SLM6031434 hydrochloride has the potential for renal fibrosis research[1][2].

  • CAS Number: 1897379-34-8
  • MF: C22H31ClF3N5O2
  • MW: 489.96
  • Catalog: SPHK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SK1-​I hydrochloride

SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM[1]. 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[2].

  • CAS Number: 2366222-05-9
  • MF: C17H28ClNO2
  • MW: 313.86
  • Catalog: SPHK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one,Sphingosine Kinase Inhibitor V

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[1][2].

  • CAS Number: 24418-86-8
  • MF: C15H10O4
  • MW: 254.24
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

erythro-ω-Amino Sphingosine Biotinamide

Biotinylated sphingosine (Biotinyl-Sph) is a substrate of sphingosine kinase that can b used to detect the phosphorylation activity of sphingosine kinase 1 (SPHK1) and SPHK2[1].

  • CAS Number: 752987-57-8
  • MF: C28H52N4O4S
  • MW: 540.80200
  • Catalog: SPHK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MP A08

MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SphK1 and SphK2 with Kivalues of 6.9 ± 0.8 μM and 27 ± 3 μM, respectively.In vitro:MP-A08 blocks pro-proliferative signalling pathways, induces mitochondrial-associated apoptosis in a SK-dependent manner, and reduces the growth of human lung adenocarcinoma tumours in a mouse xenograft model by both inducing tumour cell apoptosis and inhibiting tumour angiogenesis. MP-A08 inhibit SphK2, cause a decrease in EC barrier integrity in vitro in both cell type.[2]In vivo: MP-A08 suppresses the growth of human lung tumor xenografts in mice.

  • CAS Number: 219832-49-2
  • MF: C27H25N3O4S2
  • MW: 519.635
  • Catalog: SPHK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 717.1±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 387.5±35.7 °C

Amgen-23

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[1].

  • CAS Number: 1448706-15-7
  • MF: C23H25Cl2N3O2S
  • MW: 478.43
  • Catalog: SPHK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

K6PC-5

K6PC-5, a synthetic ceramide derivative,is a direct sphingosine kinase 1(SPHK1) activator and elicites a rapid transient increase in intracellular calcium levels. K6PC-5 is used for the researches of skin diseases involving abnormal keratinocyte, neurodegeneration and virus infection[1][2][3].

  • CAS Number: 756875-51-1
  • MF: C19H37NO4
  • MW: 343.50100
  • Catalog: SPHK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SKI-I

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[1][2].

  • CAS Number: 306301-68-8
  • MF: C25H18N4O2
  • MW: 406.43600
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

K145 (hydrochloride)

K145 is a selective SphK2 inhibitor with an IC50 of 4.30±0.06 μM , while no inhibition of SphK1 at concentrations up to 10 μM.IC50 value: 4.3 uM [1]Target: SphK2in vitro: K145 inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of 4.30±0.06 uM , while no inhibition of SphK1 at concentrations up to 10 uM was observed. Lineweaver-Burk analysis revealed a Ki of 6.4±0.7 uM for SphK2 and indicated that K145 is a substrate competitive inhibitor (with sphingosine). K145 accumulates in U937 cells, suppresses the S1P level, and inhibits SphK2. K145 also exhibited inhibitory effects on the growth of U937 cells as well as apoptotic effects in U937 cells, and that these effects may be through the inhibition of down-stream ERK and Akt signaling pathways [1].in vivo: K145 also significantly inhibited the growth of U937 tumors in nude mice by both intraperitoneal and oral administration, thus demonstrating its in vivo efficacy as a potential lead anticancer agent [2].

  • CAS Number: 1449240-68-9
  • MF: C18H25ClN2O3S
  • MW: 384.92100
  • Catalog: SPHK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PF 543 hydrochloride

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[1][2][3].

  • CAS Number: 1706522-79-3
  • MF: C27H32ClNO4S
  • MW: 502.07
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

K145

K145 is a selective SphK2 inhibitor with an IC50 of 4.30±0.06 μM , while no inhibition of SphK1 at concentrations up to 10 μM.IC50 value: 4.3 uM [1]Target: SphK2in vitro: K145 inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of 4.30±0.06 uM , while no inhibition of SphK1 at concentrations up to 10 uM was observed. Lineweaver-Burk analysis revealed a Ki of 6.4±0.7 uM for SphK2 and indicated that K145 is a substrate competitive inhibitor (with sphingosine). K145 accumulates in U937 cells, suppresses the S1P level, and inhibits SphK2. K145 also exhibited inhibitory effects on the growth of U937 cells as well as apoptotic effects in U937 cells, and that these effects may be through the inhibition of down-stream ERK and Akt signaling pathways [1].in vivo: K145 also significantly inhibited the growth of U937 tumors in nude mice by both intraperitoneal and oral administration, thus demonstrating its in vivo efficacy as a potential lead anticancer agent [2].

  • CAS Number: 1309444-75-4
  • MF: C18H24N2O3S
  • MW: 348.46000
  • Catalog: SPHK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SphK1&2-IN-1

SphK1&2-IN-1 is a SphK inhibitor targeting to SphK1 and SphK2. SphK1&2-IN-1 has thermal stability[1][2].

  • CAS Number: 1415662-57-5
  • MF: C14H14N2O3S
  • MW: 290.34
  • Catalog: SPHK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SKI-178

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 drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines[1][2].

  • CAS Number: 1259484-97-3
  • MF: C21H22N4O4
  • MW: 394.42400
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MHP

MHP is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production in KC.

  • CAS Number: 1104874-94-3
  • MF: C16H23NO4
  • MW: 293.35800
  • Catalog: SPHK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ABC294640

Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.

  • CAS Number: 915385-81-8
  • MF: C23H25ClN2O
  • MW: 380.910
  • Catalog: SPHK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 589.5±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 310.3±30.1 °C

SK1-IN-1

SK1-IN-1 is a potent sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 58 nM.

  • CAS Number: 1218816-71-7
  • MF: C22H30N4O3
  • MW: 398.499
  • Catalog: SPHK
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SK1-I (BML-258)

SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM[1]. 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[2].

  • CAS Number: 1072443-89-0
  • MF: C17H28ClNO2
  • MW: 313.86300
  • Catalog: SPHK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A