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. 2020 Jan 7;9(1):140. doi: 10.3390/cells9010140

Table 1.

SCD inhibitors used in the literature and related pathologies.

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]