Table 1.
Inhibitor | Pathology | Tissue/Organ | Dose | Effect | References |
---|---|---|---|---|---|
A939572 (Bristol-Meyer Squibb) |
Alopecia, Hypoplasia of meibomiam and sebaceous glands | Skin | 3–60 mg/Kg | Sebaceous gland atrophy, reduction of lipid content | [14] |
Cancer | Pharynx Stomach Kidney Thyroid |
19 nM 100 mg/Kg 6–65 nM 5–100 nM |
Cell growth inhibition, cell death | [38,39,40] | |
Cancer stem cells, mouse embryos Ovarian cancer Stem cells |
75–100 nM 5 μM |
Induce cell death thought ER stress, UPR Induce ferroptosis and apoptotic ceramides |
[17,41] | ||
CAY10566 (Cayman Chemical) |
Cancer | Liver Ovary Colon |
7–8 nM, 5 μM 1 μM |
Cell growth inhibition, decrease in the oleic content, alterations in autophagy | [14,42,43,44] |
Cancer stem cells | 75 nM 1–5 μM |
Reduce cell viability Reduce NFκB signaling Induce ferroptosis and apoptotic ceramides |
[17,41,42] | ||
PluriSIn#1 | Cancer | Cancer stem cells Cancer cell lines, Fibroblast, mouse embryos |
20 μM | Induce cell death thought ER stress, UPR, and ROS/NOS | [41] |
MF-438 | Cancer | Thyroid Lung |
2–5 nM | Cell growth inhibition, cell death, decrease of ALDH1A levels | [14] |
Lung cancer stem Cells Ovarian cancer Stem cells |
0.007–50 μM 1 μM |
Induce cycle arrest, apoptosis, RE stress, and autophagy Induce ferroptosis and apoptotic ceramides |
[17,45] | ||
MK-8245 (Merk Frosst) |
Type II diabetes, dyslipidemia, obesity | Liver | 20–60 mg/Kg | Antidyslipidemic Antidiabetic |
[46] |
SCDi I/II | Cancer | Breast and prostate cancer cell lines | 0.001 nM–100 μM | Cytochrome C dependent apoptosis and tumor growth inhibition | [47] |
CVT-11127 | Cancer | Lung cancer cells | 1 μM | Inhibit cell cycle and induce cell apoptosis | [48] |
XEN103 (Novartis) |
Acne | Skin | 2–14 nM | Sebaceous gland atrophy Blockage of SCD1 transcription induced by androgens Phosphatidylcholine decrease of monounsaturated acyl chains |
[14,49] |
Sterculic Acid | Metabolic syndrome | Adipose tissue Liver |
Diets supplemented with 0.4%–1.3% of SO | Blood pressure decrease, loss of body weight, decrease of serum triglyceride levels, decrease of arachidonic acid levels, improvement of glucose clearance, reduction of hepatic steatosis | [50,51,52,53] |
Parasitic diseases (toxoplasmosis, malaria, and tuberculosis) | Small intestine Erythrocytes Lungs |
870 μM–1 mM, 10–100 μg/mL | Cell cytotoxicity at high concentrations, inhibition of tachyzoites release, inhibition of oleic acid synthesis | [54,55,56] | |
Age-related macular degeneration | Retina | 1–10 μM | Counteracts the inflammatory and cytotoxic effects of 7-ketocholesterol, but seems to be independent from its capacity to inhibit SCD1 | [57,58] |