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Metabolism

ATP Citrate Lyase

(11)

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(36)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(33)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(85)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(47)

Stearoyl-CoA Desaturase (SCD)

Fatty Acid Synthase

Fatty acid synthase (FAS) is an enzyme that in humans is encoded by the FASN gene.Fatty acid synthase is a multi-enzyme protein that catalyzes fatty acid synthesis. It is not a single enzyme but a whole enzymatic system composed of two identical 272 kDa multifunctional polypeptides, in which substrates are handed from one functional domain to the next.Its main function is to catalyze the synthesis of palmitate (C16:0, a long-chain saturated fatty acid) from acetyl-CoA and malonyl-CoA, in the presence of NADPH.

Filter HomeSignaling PathwaysMetabolismFatty Acid Synthase

Denifanstat

T152711399177-37-7

Denifanstat (FASN-IN-2) is a fatty acid synthase (FASN) inhibitor (IC50=0.052 μM, EC50=0.072 μM) with selective and oral activity. Denifanstat has been used in studies of steatohepatitis.

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Rimiducid

T14298195514-63-7

Rimiducid is a lipid-permeable tacrolimus analogue, homodimerizing an analogue of human protein fkbp12 and binding to wild-type fkbp12 with 1000-fold lower affinity. Rimiducid is a dimerizer agent that acts by cross-linking the FKBP domains. It dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.

$138

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VY-3-135

T97321824637-41-3

VY-3-135 is an orally active, stable and specific acetyl-CoA synthetase 2 (ACSS2) inhibitor with IC50 of 44 nM, showing no inhibitory activity against recombinant human ACSS1 or ACSS3. VY-3-135 can effectively inhibit ACSS2-dependent fatty acid metabolism but has no effect on gene expression in tumors.

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TVB-3664

T171812097262-58-1

TVB-3664 is an orally active, selective, reversible, and highly bioavailable fatty acid synthase inhibitor (FASN) with an IC50 for palmitate synthesis of 18 nM in human and 12 nM in mouse.Significantly inhibits microtubule protein palmitoylation and mRNA expression.

$123

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Cerulenin

TQ026017397-89-6

Cerulenin is a natural inhibitor of fatty acid synthase (FAS). It is produced by the fungus Cephalosporium caeruleus.

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Orlistat

T068696829-58-2

Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.

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Ac-CoA Synthase Inhibitor1

T4380508186-14-9

Ac-CoA Synthase Inhibitor1 (ACSS2 inhibitor) is the most potent and specific inhibitor of acetate-dependent acetyl-CoA synthetase 2 (ACSS2).

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ACSS2-IN-2

T600602332820-04-7

ACSS2-IN-2 (MTB-9655) is an inhibitor of acyl-CoA synthetase short-chain family member 2 (ACSS2). ACSS2-IN-2 can inhibit ACSS2 activity with an IC50 value of 3.8 nM. ACSS2-IN-2 can be used for the research of several diseases, such as viral infection, metabolic disorders, neuropsychiatric diseases, inflammatory autoimmune conditions and cancer.

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C75

T10657218137-86-1

C75 is an inhibitor synthetic fatty-acid synthase (FASN) and inhibits prostate cancer cells PC3 (IC50: 35 μM).

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FASN-IN-1

T112671808260-84-5In house

FASN-in-1 is an effective, specific inhibitor of fatty acid synthase (FASN), a compound specifically designed to target and inhibit the activity of the enzyme involved in fatty acid synthesis, potentially disrupting fatty acid production and affecting various cellular processes.

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A-769662

T2468844499-71-4

A-769662 is an effective, reversible AMPK activator(EC50=0.8 μM).

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TVB-3166

T171801533438-83-3

TVB-3166 induces apoptosis and inhibits in-vivo xenograft tumor growth. TVB-3166 is a reversible and selective fatty acid synthase inhibitor (IC50s: 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively).

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Beta-Hydroxyisovalerylshikonin

TN14407415-78-3

Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg mL).

$139

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IPI-9119

T368411346564-56-4

IPI-9119 is an orally active, selective, and irreversible FASN inhibitor (IC50 = 0.3 nM).

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trans-C75

T10656191282-48-1

trans-C75 ((±)-C75) is an enantiomer of C75, which is an inhibitor of fatty-acid synthase (FASN).

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Lycorine

T3324476-28-8

Lycorine (Narcissine) inhibits protein synthesis and may inhibit ascorbic acid biosynthesis, although studies on the latter are controversial and inconclusive.

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Fatostatin

T9266125256-00-0

Fatostatin is a specific inhibitor of SREBP activation, it impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs.

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Fatostatin hydrobromide

T6832298197-04-3

Fatostatin hydrobromide (Fatostatin A HBr) ia an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.

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Isoscoparin

TN180320013-23-4

Isoscoparin is derived from Gentiana algida Pall with antioxidant and anti-adipogenic activities. Isoscoparin can be used in stuides about the prevention and treatment of obesity.

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UCM05

T218311094451-90-7

UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) with efficacy against HER2+ breast cancer xenografts, including cell lines resistant to anti-HER2 drugs [1]. Additionally, it functions as an inhibitor of the Filamentous temperature-sensitive protein Z (FtsZ), selectively inhibiting the growth of the Gram-positive bacterium B. subtilis with minimum inhibitory concentration (MIC) values of 100 μM, while showing no activity against the Gram-negative bacterium E. coli [2].

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Pyrazinamide

T142698-96-4

Pyrazinamide (Pyrazinecarboxamide), an antimycobacterial, is utilized therapeutically as an antitubercular agent, which is a synthetic pyrazinoic acid amide derivative.

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Pedunculoside

T282442719-32-4

Pedunculoside is extracted from Ilex rotunda Thunb.

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FT113

T79471630808-89-7

FT113 is a novel potent inhibitor of fatty acid synthase (fasn, IC50 : 213 nM),and exhibits anti-cancer activity

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Trimetazidine dihydrochloride

T098813171-25-0

Trimetazidine dihydrochloride (Vastarel F) can improve myocardial glucose utilization by inhibiting fatty acid metabolism. Trimetazidine is the first cytoprotective anti-ischemic agent, also used as a vasodilator in ischemic heart disease or angina.

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Fasnall HCl

T27307L

Fasnall HCl is a selective FASN inhibitor that acts through its co-factor binding sites. Fasnall HCl also shows potent anti-tumor activity in the MMTV-Neu model of HER2(+) breast cancer, particularly when combined with carboplatin.

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trans-Chalcone

T3322614-47-1

trans-Chalcone (Chalkone) is an aromatic ketone that forms the central core for a variety of important biological compounds, which are known collectively as chalcones.

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Fasnall

T27307929978-58-5

Fasnall is a selective FASN inhibitor that acts through its co-factor binding sites. Fasnall shows potent anti-tumor activity in the MMTV-Neu model of HER2(+) breast cancer, particularly when combined with carboplatin.

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Fas C-Terminal Tripeptide Acetate

T21724L

Fas C-Terminal Tripeptide Acetate shows inhibitory activity of Fas/FAP-1 binding.

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FGH10019

T77981046045-61-7

FGH10019 is a novel inhibitor of sterol regulatory element-binding protein (SREBP) ( IC50 :1 μM).

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FASN-IN-3

T115572097262-60-5

FASN-IN-3 is an inhibitor of fatty acid synthase (FASN).

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BI 99179

T145701291779-76-4

BI 99179 is a selective and potent inhibitor of type I fatty acid synthase (FAS), a tool compound for targeting FAS for cancer research.

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Pseudoprotodioscin

T5S0246102115-79-7

1. Pseudoprotodioscin has moderate cytotoxicity.

$130

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GSK2194069

T154291332331-08-4

GSK2194069 is an active β-keto reductase (KR)-specific inhibitor of fatty acid synthase (FASN) with an IC50 of 7.7 nM in an assay for the detection of released CoA.GSK2194069 inhibits the proliferation of FAS in cancer cells through the action of acetoacetyl-coenzyme A and NADPH.

$149

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Hydroxycitric acid

TN17516205-14-7

(-)-Hydroxycitric acid (HCA) can inhibit fat synthesis and reduces food intake, the primary mechanism of action of HCA appears to be related to its ability to act as a competitive inhibitor of the enzyme ATP-citrate lyase, which catalyzes the conversion of citrate and coenzyme A to oxaloacetate and acetyl coenzyme A (acetyl-CoA), primary building blocks of fatty acid and cholesterol synthesis.

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Icariside E4

TN5431126253-42-7

Icariside E4 is a natural compound derived from Ulmus minor that acts via AMPK phosphorylation and inhibition of MID1IP2 hypolipidation in HepG1 cells.Icariside E4 has anti-injurious, antioxidant, anti-Alzheimer's and anti-inflammatory effects and inhibits SREBP-1c, liver X receptor-α (LXR) and FASN in Icariside E4 is an effective candidate for the treatment of fatty liver disease and has hypolipidemic potential in HepG1 cells.

$1,620

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Albaspidin AP

TN136559092-91-0

Albaspidin-AP, -PP, -PB inhibit Fatty acid synthase (FAS) with IC50 values ranging from 23.1+ -1.4 to 71.7+ -3.9 microM, they could be considered to be a promising class of FAS inhibitors, and FAS is emerging as a potential therapeutic target to treat can

$410

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Gallocatechin gallate

TN40945127-64-0

Gallocatechin gallate has strong antioxidative, and anti-obesity activities, it inhibits 3T3-L1 differentiation and lipopolysaccharide induced inflammation through MAPK and NF-ÎºB signaling; it also may have anti-diabetic effects by increasing sensitivity

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1-Hydroxy-2-oxopomolic acid

TN2535217466-37-0

1β-Hydroxy-2-oxopomolic acid inhibits adipocyte differentiation through downregulation of various adipocytokines by blocking PPARγ and C/EBPα expression.

$740

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FAS-IN-1 Tosylate

T11266L

FAS-IN-1 Tosylate is an effective fatty acid synthase inhibitor;Has an IC50 of 10 nM.

$171

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