| S7174 |
Opaganib (ABC294640)
|
Opaganib (ABC294640) is an orally bioavailable and selective sphingosine kinase-2 (SphK2) inhibitor with IC50 of approximately 60 μM. This compound is in Phase 1/2.
|
-
Sci Rep, 2025, 15(1):4152
-
Cell Res, 2022, 10.1038/s41422-022-00614-0
-
Bioact Mater, 2022, 15:29-43
|
|
| S7177 |
PF-543 hydrochloride
|
PF-543 hydrochloride, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. This compound induces apoptosis, necrosis, and autophagy.
|
-
Cell Death Discov, 2025, 11(1):29
-
FASEB J, 2025, 39(12):e70768
-
FASEB J, 2025, 39(12):e70768
|
|
| S7176 |
SKI II
|
SKI II (SphK-I2) is a highly selective and non ATP-competitive sphingosine kinase (SphK) inhibitor with IC50 of 0.5 μM, while this compound exhibits no inhibitory action on other kinases including PI3K, PKCα and ERK2.
|
-
Transl Cancer Res, 2025, 14(5):2594-2602
-
Clin Transl Med, 2022, 12(2):e695
-
Int J Biol Sci, 2022, 18(7):2994-3005
|
|
| S0817 |
SKI-V
|
SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. This compound also inhibits PI3K with IC50 of 6 μM for hPI3k. It decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity.
|
-
Cell Death Discov, 2022, 8(1):48
-
Cell Death Discov, 2022, 8(1):48
|
|
| S6512 |
Defensamide (MHP)
|
Defensamide (MHP) is an activator of sphingosine kinase (SPHK1) that modulates the innate epidermal immune response by potentiating SPHK1 activity and inducing cAMP production.
|
-
bioRxiv, 2025, 2024.08.06.606815
|
|
| E1218 |
K6PC-5
|
K6PC-5, a ceramide derivative, is a sphingosine kinase 1 (SPHK1) activator and elicits a rapid transient increase in intracellular calcium levels.
|
-
Cell Prolif, 2024, e13604.
-
Int J Biol Sci, 2022, 18(7):2994-3005
|
|
| S5989 |
SKI-178
|
SKI-178 is a potent inhibitors of sphingosine kinase-1 (SphK1) and SphK2 with IC50 values ranging from ∼500 nM to ∼1 μM depending on AML cell lines.
|
|
|