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
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H9030 |
YHR17 |
2392996-74-4 | YHR17 is a potent sphingosine kinase 1(SphK1) inhibitor with IC50 values that ranged from 0.68 to 5.68μM and inhibited the proliferation of the A375 cell line by affecting the cell cycle and apoptosis. Furthermore, YHR17 inhibited SphK1 with more than 125-fold selectivity over SphK2. |
H9028 |
YHR1 |
2378647-14-2 | YHR1 is a potent sphingosine kinase 1 and 2 (SphK1/2) inhibitor with IC50 >100 μM. |
H9027 |
CHJ01 |
CHJ01 is a potent sphingosine kinase 1 and 2 (SphK1/2) inhibitor with IC50 value of 8.9 μM,and better anti-RA effect; CHJ01 showed an anti-inflammatory effect similar to that of MTX in vitro, its IC50 value is 8.64 μM. |
|
H4076 |
SKI-178 |
1259484-97-3 | SKI-178 is a potent, specific, non-lipid SphK1 inhibitor with Ki of 1.33 uM, displays no significant activity for SphK2 (IC50>25 uM); induces apoptosis in human AML cell lines in a CDK1-dependent manner and is not a substrate for MDR1; shows effectivity in mouse models of AML. |
H4075 |
RB-005 |
1425049-20-2 | RB-005 (RB-005) is a potent, selective inhibitor of sphingosine kinase SphK1 (SK1) with IC50 of 3.6 uM, displays 15-fold selectivity over SphK2. |
H4074 |
PF-543 |
1415562-82-1 |
PF-543 (PF543) is a potent, specific, cell-permeant inhibitor of SphK1 with Ki of 3.6 nM, displays >100-fold selectivity over the SphK2 isoform; decreases the level of endogenous S1P 10-fold with a proportional increase in the level of sphingosine in 1483 head and neck carcinoma cells; reduces sickling, hemolysis, and inflammation in SCD Tg mice by reducing erythrocyte SPHK1 activity and S1P levels; induces apoptosis, necrosis, and autophagy in human head and neck SCC cells. |
H4073 |
Opaganib |
915385-81-8 |
Opaganib (ABC-294640, ABC294640) is a selective, competitive and orally bioavailable sphingosine kinase-2 (SphK-2) inhibitor with IC50 of 60 uM, Ki of 9.8 uM; shows no activity against SphK-1 with IC50 of >100 uM; attenuates S1P formation in intact cells, suppresses the proliferation of a broad panel of tumor cell lines, and inhibits tumor cell migration concomitant with loss of microfilaments; demonstrates antitumor activity in adenocarcinoma xenograft models. |
H4072 |
MP-A08 |
219832-49-2 | MP-A08 is a first-in-class, highly selective, ATP competitive sphingosine kinase (SphK) inhibitor (Ki of 6.9/27 uM for SK2/SK1); inhibits S1P production and increases pro-apoptotic sphingolipids in Jurkat cells; reduces the growth of human lung adenocarcinoma tumours in a mouse xenograft model by both inducing tumour cell apoptosis and inhibiting tumour angiogenesis. |
H4071 |
Fingolimod hydrochloride |
162359-56-0 | Fingolimod (FTY 720) is an immunomodulatory agent can be phosphorylated by SphK, then functions as a potent agonist of S1P receptors (S1P1/3/4/5) with EC50 of 0.3-5 nM; has no affitnity for S1P2; alters lymphocyte trafficking and inhibits lymphocyte recirculation. |
H4070 |
ABC 294640 hydrochloride |
1185157-59-8 |
ABC 294640 (ABC294640, Opaganib)?is a selective, competitive and orally bioavailable sphingosine kinase-2 (SphK-2) inhibitor with IC50 of 60 uM, Ki of 9.8 uM; shows no activity against SphK-1 with IC50 of >100 uM; attenuates S1P formation in intact cells, suppresses the proliferation of a broad panel of tumor cell lines, and inhibits tumor cell migration concomitant with loss of microfilaments; demonstrates antitumor activity in adenocarcinoma xenograft models. |
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