Name |
Mechanism |
Disease |
References |
FTY720 (Fingolimod,Gilenya) |
-Prodrug; phosphorylated by SphK2. -S1PR1, S1PR3-5 agonist - Downregulates S1P1 |
-FDA approved for multiple sclerosis* -Dermatitis, Arthritis, Allergy |
[13,80] |
SK1-1 (BML-258) |
-SphK1 inhibitor |
-Glioblastoma -Leukemia |
[114,115] |
Safingol L-threo-dihydrosphingosine |
-pan SphK inhibitor |
-Solid tumors(Phase 1)* |
[116] |
SK1-2 |
SphK1 inhibitor Induces proteasomal and lysosomal degradation of SphK1 |
-Pancreatic cancer -Leukemia |
[117,118] |
ABC294640 |
SphK2 inhibitor Estrogen receptor agonist |
-Cancer -Inflammatory bowel disease |
[119,120] |
ABC294735 |
pan SphK inhibitor |
-Cancer |
[121] |
SKI-II (SKI-2, SPHK I2) |
SphK1 inhibitor |
-Asthma |
[122] |
THI 2-acetyl-4(5)-[1(R) |
S1P Lyase inhibitor |
-Ischemia/reperfusion injury |
[123] |
LX2931 |
S1P Lyase inhibitor |
-Rheumatoid arthritis(Phase II) * |
[124] |
SKI 5C |
SphK1 inhibitor |
-Sepsis |
[125] |
SEW2871 |
S1PR1 agonist |
-Diabetic nephropathy -Renal protection |
[126,127] |
JTE013 |
S1PR2 antagonist |
-Anaphylaxis -Cancer |
[128] [71] |
AAL® |
Prodrug; phosphorylated by SphK2 S1PR1/S1PR3 agonist |
-Influenza |
[129] |
AUY954 |
S1PR1 agonist |
-Experimental autoimmune neuritis |
[130] |