desaturase

PDS-IN-1 potently inhibits Oryza sativa phytoene desaturase (OsPDS), exhibiting herbicidal activity [1].

Phytoene desaturase-IN-1, a potent inhibitor of phytoene desaturase (PDS) with a dissociation constant (Kd) of 65.9 μM, acts through π−π stacking interaction with the Phe301 residue. This compound exhibits a broad spectrum of post-emergence herbicidal effects by inducing a reduction in PDS mRNA, and accumulation of phytoene and reactive oxygen species (ROS) in albino leaves, suggesting its utility in agricultural production [1].

SW209049 is a stearoyl-CoA 9-desaturase inhibitor. SW209049 exhivits potent activity against H2122 cell with IC50 of 0.13uM.

MK-8245 analog is an analog of MK-8245 which is a liver-targeted Inhibitor of Stearoyl-CoA Desaturase (SCD). It is useful for the Treatment of Dyslipidemia and Diabetes.

GSK1940029 (SCD inhibitor 1) is a stearoyl-coa desaturase (SCD) inhibitor.

Sterculic acid, a stearoyl-CoA desaturase-1 (SCD1) inhibitor, effectively suppresses delta-9 desaturase (Δ9D) activity in a dose-dependent manner, exhibiting an inhibition concentration (IC50) value of 0.9 μM [1].

A939572 is stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM for mSCD1 and 37 nM for hSCD1.

Elemicin (Elemicine) is a constituent of several plant species' essential oils with anticholinergic effects in human.

Sesamin is a selective delta 5 desaturase inhibitor in the biosynthesis of polyunsaturated fatty acids and is a lignan abundantly present in sesame oil. It has potent neuroprotective effects against cerebral ischemia.

PluriSIn 1 (NSC 14613) is an inhibitor of stearoyl-CoA desaturase (SCD1), the key enzyme in oleic acid biosynthesis, revealing a unique role for lipid metabolism in hPSCs.

Jacaric acid is a conjugated polyunsaturated fatty acid first isolated from seeds of Jacaranda plants. Structurally, it is an 18-carbon ω-6 triene isomer of γ-linolenic acid . Jacaric acid induces cell cycle arrest and apoptosis in a variety of cancer cell lines (GI50 = 1-5 μM). It increases the production of reactive oxygen species, and cytotoxicity is abolished by the antioxidant α-tocopherol, suggesting that apoptosis results from oxidative stress. Jacaric acid is metabolized in vivo to conjugated linoleic acid , which is also cytotoxic to cancer cells. Jacaric acid inhibits cyclooxygenase-1 in vitro (Ki = 1.7 μM) and, with long term feeding, decreases stearoyl-CoA desaturase expression and activity in mice.

C24 dihydro Ceramide is a sphingolipid that has been found in the stratum corneum of human skin.[1] It is found in higher concentrations in female sebum compared to male sebum.[2] C24 dihydro Ceramide levels positively correlate with cytotoxicity in CCRF-CEM, MOLT-4, COG-LL-317h, and COG-LL-332h T cell acute lymphoblastic leukemia (ALL) cell lines.[4] Levels of C24 dihydro ceramide are increased by 149.49-fold in dihydroceramide desaturase 1 (DEGS1) knockdown UM-SCC-22A human head and neck squamous carcinoma cells in vitro.[4] C24 dihydro Ceramide levels are also increased in INS-1 β-cells incubated with glucose and palmitate.[5]

9(Z),12(Z),15(Z),18(Z),21(Z)-Tetracosapentaenoic acid is an ω-3 very long-chain polyunsaturated fatty acid. It has been used to study the desaturation and elongation of ω-3 polyunsaturated fatty acids. It is elongated to form C26:5 or acted on by δ6 desaturase to form C24:6. 9(Z),12(Z),15(Z),18(Z),21(Z)-Tetracosapentaenoic acid is found at low levels in mouse brain and spleen and levels decrease in the brain and spleen of old and exceptionally old mice.

Beflubutamid is an herbicide. It works by inhibiting phytoene-desaturase.

XEN103 is a potent and selective Stearoyl-CoA Desaturase-1 inhibitor.

T-3364366 is an inhibitor of thienopyrimidinone delta-5 desaturase (Δ5D) with IC50s of 1.9 nM and 2.1 nM in HepG2 and RLN-10 cells, respectively.

MK-8245 trifluoroacetate is a phenoxy piperidine isoxazole derivative functioning as a potent, liver-targeting stearoyl-CoA desaturase (SCD) inhibitor, demonstrating significant anti-diabetic and anti-dyslipidemic effects. It showcases high specificity and efficacy against SCD1 across various species, with IC50 values of 1 nM for human SCD1 and 3 nM for both rat and mouse SCD1. MK-8245's mechanism includes a tetrazole acetic acid moiety that facilitates liver-targeting through OATPs recognition. Its inhibition potency in rat hepatocyte assays (IC50 of 68 nM) surpasses that in HepG2 cell assays devoid of active OATPs (IC50 of ~1 μM), highlighting its liver specificity. Moreover, MK-8245 exhibits over 100,000-fold selectivity against Δ-5 and Δ-6 desaturases in comparative assays. In vivo studies reveal MK-8245's preferential liver distribution in mice, rats, dogs, and rhesus monkeys, underscoring its potential for minimizing adverse effects in non-target tissues. Additionally, its administration in eDIO mice before glucose challenges significantly improves glucose clearance, indicating its therapeutic promise in diabetes management.

5-Dehydroepisterol is an episterol derivative with anti-fungal activities. It can be formed by C-5 sterol desaturase and converted into 24-methylenecholesterol by 7-dehydrocholesterol reductase.

gamma-Linolenic acid (gamolenic acid), is an unsaturated fatty acid synthesized from linoleic acid (LA) by the enzyme delta-6-desaturase. Research on hepatocellular cell lines has shown γ-Linolenic Acid to have induced reactive oxygen species generation including lipid peroxidation, cell growth inhibition, and heme oxygenase-1 production for antioxidant protection against oxidative stress. Further experiments have noted that γ-Linolenic acid inhibits inflammatory responses through inactivation of NFκB and activator protein-1 by suppressed oxidative stress.

8(E),10(E),12(Z)-Octadecatrienoic acid is a conjugated polyunsaturated fatty acid (PUFA) that has been found inC. officinalisseed oil and has anticancer activity.1,2,3It inhibits the growth of Caco-2 cells when used at concentrations ranging from 10 to 50 μM.28(E),10(E),12(Z)-Octadecatrienoic acid (10 μM) induces formation of thiobarbituric acid reactive substances (TBARS) and apoptosis in DLD-1 colorectal adenocarcinoma cells.3It also inhibits prostaglandin biosynthesis in sheep vesicular gland microsomes (IC50= 31 μM).4 1.Crombie, L., and Holloway, S.J.The biosynthesis of calendic acid, octadeca-(8E,10E, 12Z)-trienoic, acid, by developing marigold seeds: origins of (E,E,Z) and (Z,E,Z) conjugated triene acids in higher plantsJ. Chem. Soc. Perk. T. 12425-2434(1985) 2.Yasui, Y., Hosokawa, M., Kohno, H., et al.Growth inhibition and apoptosis induction by all-trans-conjugated linolenic acids on human colon cancer cellsAnticancer Res.26(3A)1855-1860(2006) 3.Shinohara, N., Ito, J., Tsuduki, T., et al.Jacaric acid, a linolenic acid isomer with a conjugated triene system, reduces stearoyl-CoA desaturase expression in liver of miceJ. Oleo Sci.61(8)433-441(2012) 4.Nugteren, D.H., and Christ-Hazelhof, E.Naturally occurring conjugated octadecatrienoic acids are strong inhibitors of prostaglandin biosynthesisProstaglandins33(3)403-417(1987)

SCD1 inhibitor-1 is a potent and liver-selective inhibitor of stearoyl-CoA desaturase-1 (SCD1).

GT-11 is an inhibitor of dihydroceramides (DHCer) desaturase activity.

D5D-IN-326 is an orally active delta-5 desaturase (D5D) inhibitor (IC50s: 72 and 22 nM for rat and human D5D in enzymic and cell-based assays). It has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in die

CP-24879 hydrochloride (CP-24879 HCl), a Δ5D/Δ6D dual-inhibitor, can significantly reduce intracellular lipid accumulation and inflammatory injury in hepatocytes. CP-24879 hydrochloride exhibits superior antisteatotic and anti-inflammatory actions in fat-1 and ω-3-treated hepatocytes.

SCD1 inhibitor-4 is stearoylCoA desaturase-1 (SCD1) inhibitor. SCD1 inhibitor-4 can be used for the research of diabetes.

CVT-12012 is an orally bioavailable inhibitor of stearoyl-CoA desaturase (SCD; IC50 = 6.1 nM in HepG2 cells).

CAY10566 shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM). CAY10566 is a potent, orally bioavailable and selective stearoyl

T-3764518 is a novel and potent inhibitor of stearoyl coenzyme A desaturase (SCD)(IC50 of 4.7 nM).

SW203668 is an irreversible inhibitor of stearoyl-CoA desaturase (IC50 = 54 nM). It is selectively cytotoxic to H2122, H460, HCC44, and HCC95 cell lines that express cytochrome P450 (CYP) isoform CYP4F11 over eight other cancer cell lines that lack CYP4F11 in vitro (IC50s = 22-116 and >10,000 nM, respectively) and ectopic expression of CYP4F11 in SW203668-insensitive H1155 cells results in sensitization to SW203668. In vivo, SW203668 reduces tumor growth rate without reducing sebocyte production in the H2122 wild-type and nonobese diabetic severe combined immunodeficiency (NOD-SCID) mouse xenograft models when administered at doses of 20 and 6 mg/kg, respectively.

Docosapentaenoic acid (DPA), a 22-carbon fatty acid primarily found in fish oil, constitutes a minor fraction of the total unsaturated fatty acids in human serum, with concentrations ranging from 0.1% to 1%, which can increase through dietary supplementation. The all-cis-4,7,10,13,16-DPA variant, also known as Austrian acid, represents a specific isomer of DPA and falls into the omega-6 category, synthesized through the elongation and desaturation of arachidonic acid. In conditions such as fatty acid desaturase syndrome, its levels may decrease, potentially influencing development. Furthermore, conditions like nonalcoholic steatohepatitis, a precursor to hepatocellular carcinoma, are marked by enhanced expression of the hepatic elongase very long fatty acid protein 6 and increased concentrations of very long-chain fatty acids, including all-cis-4,7,10,13,16-DPA.

CVT-11127 is an StearoylCoA Desaturase-1 (SCD1) inhibitor.

Fluridone (EL-171) is a potent inhibitor of abscisic acid (ABA) synthesis, inhibits the expression of AchnFAR and TF genes, and reduces the formation of primary alcohol. Fluridone is often used as an aquatic herbicide to control invasive plants and is also used to control species such as hydra and Eurasian hydra.

YTX-465 is an inhibitor of both stearoyl-CoA desaturase(IC50s = 39 nM) and Ole1 (IC50s = 30.4 μM).

SW208108 is a tumor-specific irreversible inhibitor of stearoyl CoA desaturase (SCD).

All-cis-4,7,10,13,16-Docosapentaenoic acid (all-cis-4,7,10,13,16-DPA) methyl ester, also known as Osbond acid, is an isomer of DPA and a more lipid-soluble variant of the free acid, primarily found in fish oils as an ω-3, 22-carbon fatty acid. Despite being an ω-6 fatty acid synthesized through the elongation and desaturation of arachidonic acid, its levels can decrease due to fatty acid desaturase syndrome, potentially impacting development. Additionally, increased expression of hepatic elongation of very long fatty acids protein 6 and elevated levels of very long-chain fatty acids, including all-cis-4,7,10,13,16-DPA, are indicative of nonalcoholic steatohepatitis, a condition that precedes hepatocellular carcinoma.

MK-8245 is a liver-targeting SCD inhibitor for human SCD1 (IC50: 1 nM) and for rat/mouse SCD1 (IC50: 3 nM), with anti-diabetic and anti-dyslipidemic function.

Diflufenican (M&B 38544) increases the production of phytoene in carrot cell cultures by inducing the inhibition of phytoene desaturase gene expression.

SSI-4 is a Stearoyl CoA desaturase 1 (SCD1) inhibitor that can be labeled with carbon-11 (11C) for use as a ligand in small animal in vivo PET/CT imaging studies of SCD1 [1].

Sterculic acid methyl ester, an ester derivative of sterculic acid known for inhibiting Δ9 desaturase, has been found to adversely affect and exhibit toxicity towards R. opacus bacteria at a concentration of 0.75 mM. It not only hampers bacterial growth but also modifies fatty acid composition by reducing stearate and oleate levels, increasing the palmitate ratio, and decreasing overall fatty acid content at 0.25 or 0.5 mM concentrations. Additionally, at 50 ppm, Sterculic acid methyl ester enhances the tumor growth-promoting effects of aflatoxin Q1 in rainbow trout, indicating a synergistic interaction between the two compounds. [Matreya, LLC. Catalog No. 1236]

N'-(2-Fluorophenyl)pyrazine-2-carbohydrazide is a Ole1p desaturase inhibitor as well as antifungal agent [1].

SC-26196 is an orally active inhibitor of Delta6 desaturase (D6D) with IC50 of 0.2 µM in a rat liver microsomal assay, with antiinflammatory properties.

MF-438 is an effective and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor (EC50: 2.3 nM for rSCD1).

XEN723 is a potent thiazolylimidazolidinone Stearoyl-CoA Desaturase (SCD1) inhibitor(IC50s of 45 and 524 nM in mouse and HepG2 cell, respectively).