Table 3.
SphK inhibitors tested in human cancer cells and primary human cancer cells.
| SPHK Inhibitor | Cancer Cell Type | SphK Selectivity | References |
|---|---|---|---|
| B5354-c | Prostate (LNCaP, Du145 and PC-3) | SphK1 | [45,154] |
| Breast (MDA-MB-231) | |||
| F-12509a | Leukaemia (HL-60, LAMA-84 and HL-60 MDR) | SphK1 | [155] |
| Chronic Myeloid Leukaemia blasts | |||
| SK1-I | Glioma (U87MG, LN229 and U373) and Primary Glioma Cells (GBM6) | SphK1 | [36,129,156,157,158,159] |
| Leukaemia (U937, HL-60 and Jurkat) and Acute Myeloid Leukaemia blasts | |||
| Breast cancer (MDA-MB-231, MCF-7 and MCF-7 HER2) | |||
| Prostate (LNCaP) | |||
| SKI-II | Prostate (LNCaP, C4-2B and PC-3) | SphK1 and SphK2 | [43,160,161,162,163] |
| Pancreas (Panc-1 and BXPC-3) | |||
| Bladder (T24) | |||
| Breast (MCF7) | |||
| ABC294640 | Pancreatic (clinical trial) and (Panc-1) | SphK2 | [163,164,165] |
| Colorectal (HT-29 and Caco-2) | |||
| Breast (MCF-7, MDA-MB-231) | |||
| Ovarian (SK-OV-3) | |||
| Prostate (DU145) | |||
| Kidney (A-498) | |||
| Melanoma (1025LU) | |||
| Bladder (T24) | |||
| Liver (Hep-G2) | |||
| Safingol | Solid tumors (clinical trial) | SphK1 and SphK2 | [8,165,166] |
| Glioblastomas | |||
| Colorectal tumor | |||
| Colorectal (HCT116) | |||
| Adrenal cortical carcinoma | |||
| Sarcoma | |||
| N,N-dimethyl-d-erythro-sphingosine (DMS) | Lung (A549) | SphK1 and SphK2 | - |
| Acute myeloid leukemia (HL-60, U937, CMK7) | [167,168,169,170,171,172,173] | ||
| Chronic myeloid leukemia (JFP1, K562) | [174] | ||
| Gastric (MKN45, MKN74, Kato III) | [175,176] | ||
| Acute lymphoid leukemia (Jurkat) | [177,178] | ||
| Lung (LU65, NCI-1169) | [175] | ||
| Cervix carcinoma (KB-3-1) | [179] | ||
| Colon (Colo205, SW48, SW403, SW1116, SW1417, HT29, LS174T, LS180, HRT18) | [169,175] | ||
| Pheochromocytoma (PC-12) | [180,181] | ||
| Prostate adenocarcinoma (LNCaP) | [182] | ||
| Melanoma (M1733, F10, F1, BL6) | [175] | ||
| Hepatoma (Hep3B) | [183] | ||
| Epidermoid carcinoma (A431) | [169,175] | ||
| Breast adenocarcinoma (MCF7) | [184] | ||
| l-threo-dihydrosphingosine (DHS) | Acute myeloid leukemia (HL-60, P388, U937, NB4) Lymphoma (WEHI-231) | SphK1 and SphK2 | [171,172,185,186] |
| Breast adenocarcinoma (MCF7) | [187,188] | ||
| Hepatoma (Hep3B) | [183] | ||
| Neuroblastoma (SH-SY5Y) | |||
| Melanoma (A2058, 939, C8161) | [188] | ||
| FTY720 (fingolimod) | Prostate (PC-3, LNCaP-C4-2B, and DU145) | SphK1 | [189,190,191,192,193] |
| Ovarian cancer (OV2008, IGROV-1, A2780, SKOV-3, R182) | |||
| Bladder (T24, UMUC3 and HT1197) | |||
| Glioblastoma (U251MG and U87MG) | |||
| Hepatoma (HepG2, Huh-7 and Hep3B) | |||
| K145 | Leukemia (U937) | SphK2 | [194] |