Acetyl-CoA Carboxylase

Firsocostat (ND-630; GS-0976; NDI-010976) is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC₅₀ values of 2.1 and 6.1 nM, respectively.

TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).

ND-646 is an orally bioavailable and steric inhibitor of acetyl-CoA carboxylase (ACC) with IC₅₀s of 3.5 nM and 4.1 nM for recombinant hACC1 and hACC2, respectively.

VY-3-135 is a potent, orally active, and stable ACSS2 inhibitor with an IC₅₀ value of 44 nM. VY-3-135 is specific to ACSS2 among the AcCoA synthetase family of enzymes. VY-3-135 does not inhibit ACSS1 or ACSS3 enzymatic activity. VY-3-135 can be used for the research of breast cancer.

CMS-121 is a quinolone derivative and an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor. CMS-121 protects HT22 cells against ischemia and oxidative damage with EC₅₀ values of 7 nM and 200 nM, respectively. CMS-121 has strong neuroprotective, anti-inflammatory, antioxidative and renoprotective activities.

AMPK activator 18 is a potent allosteric activator of AMPK complexes containing the β2 isoform. AMPK activator 18activates α2-containing AMPK α2β2γ1 and α2β2γ3 complexes, with EC₅₀ values of 17.2 and 82.1 nM. AMPK activator 18 stimulates β2-AMPK in cells, and glucose uptake by isolated skeletal muscle. AMPK activator 18 induces acetyl-coenzyme A carboxylase (ACC) and AMPK α-T172 phosphorylation. AMPK activator 18 can be used for the research of type 2 diabetes.

PF-05221304 tromethamine is an orally active, liver-directed and dual ACC1/ACC2 inhibitor with IC₅₀s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2. PF-05221304 tromethamine is a substrate for organic anion transport polypeptides. PF-05221304 tromethamine directly improves a variety of non-alcoholic fatty liver (NAFL) and non-alcoholic steatohepatitis (NASH) pathogenic factors.

Fluazifop-d₃ is the deuterium labeled Fluazifop (HY-121427). Fluazifop is a grass-selective herbicide via inhibiting acetyl-CoA carboxylase.

PF-05175157 is broad spectrum acetyl-CoA carboxylase (ACC) inhibitor with IC₅₀s of 27.0, 33.0, 23.5 and 50.4 nM for ACC1 (human), ACC2 (human), ACC1 (rat), ACC2 (rat), respectively.

CP-640186 is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC₅₀s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 can also stimulate muscle fatty acid oxidation.

Alisol A is an orally active tetracyclic triterpenoid compound of the prototerpane type. Alisol A can be extracted from the rhizome of Alisma orientale. Alisol A activates AMPK/ACC/SREBP-1c, SIRT1, PPARα, inhibits MMP-2/-9, decreases inflammatory cytokine expression (IL-1β, IL-6, IL-8). Alisol A has anti-tumor activity against breast cancer and colorectal cancer. Alisol A has anti-obesity and anti-atherosclerotic activities. Alisol A can be used in the research of hepatitis B, breast cancer, colorectal cancer, atherosclerosis, and obesity.

Rebaudioside D is an orally active sweetener that targets and activates FXR, modulates Acetyl-CoA Carboxylase, and inhibits 3-hydroxy-3-methylglutaryl-CoA reductase. Rebaudioside D regulates bile acid homeostasis and lipid metabolism, reduces the synthesis rates of fatty acids and cholesterol, and exerts multiple effects including anti-adipogenesis, hepatoprotection, anti-steatosis, gut microbiota modulation, enhancement of secondary bile acid metabolism, anti-endotoxin activity, regulation of bile acid transport, and inhibition of bile acid efflux. Rebaudioside D also reduces body weight gain, visceral fat accumulation, hepatic triglyceride and cholesterol accumulation, hepatic lipid peroxidation, and decreases the circulating level of lipopolysaccharide-binding protein. Rebaudioside D additionally enhances the secondary bile acid metabolic pathway of intestinal bacteria, upregulates the gene expression of ileal organic solute transporter α, and downregulates the gene expression of hepatic bile salt export pump. Rebaudioside D does not affect glucose homeostasis, alter total caloric intake or fecal energy excretion, induce weight gain, exacerbate obesity, promote hepatic steatosis, impair brown adipose tissue function, nor change skeletal muscle metabolism-related proteins. Rebaudioside D can be used in diet-induced obesity and obesity-related research.

A-908292 is a potent and selective acetyl-CoA carboxylase 2 (ACC2) inhibitor, with an IC₅₀ of 23 nM for human ACC2. A-908292 can be used for the research of fatty acid metabolism. A-908292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC₅₀s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 hydrochloride can also stimulate muscle fatty acid oxidation.

Clitorin is an orally active flavonoid compound that can be isolated from Carica papaya. Clitorin is an inhibitor of EGFR (IC₅₀: 89.58 nM) and aromatase (IC₅₀: 77.41 nM). Clitorin has antioxidant and anti-tumor activities. In the DPPH and ABTS radical scavenging assays, Clitorin has IC₅₀ values of 91.96 ppm and 250.45 ppm, respectively. In addition, Clitorin can regulate lipogenesis and fatty acid oxidation and can be used in the research of non-alcoholic fatty liver disease.

MK-4074 is a liver-specific inhibitor of acetyl-CoA carboxylase ACC1 and ACC2 with IC₅₀ values of approximately 3 nM.

AD-5584 is an ACSS2 inhibitor with blood-brain permeability. AD-5584 can significantly reduce lipid storage, reduce colony formation, and increase cell death. AD-5584 has antitumor activity.

MEDICA16 is an orally active acetyl-CoA carboxylase and ATP-citrate lyase inhibitor. MEDICA16 limits the acetyl-CoA supply for acetyl-CoA carboxylase, inhibits acetyl-CoA carboxylase activity, exerts citrate-competitive inhibitory effects on ATP-citrate lyase, and reduces hepatic AMPK activity. MEDICA16 can be used in research related to insulin resistance, hyperlipidemia, and obesity.

Spiromesifen (BSN 2060) is a broad-spectrum tetrachloro acid derivative acaricide. Spiromesifen reduces lipid biosynthesis via inhibition of acetyl-CoA carboxylase, and has no cross-resistance to any resistant mite or whitefly populations.

Olumacostat glasaretil (DRM01) is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC).