Acetyl-CoA Carboxylase Inhibitor

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.

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.

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.

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).

Fluazifop-P-butyl is an orally active herbicide and ACCase inhibitor. Fluazifop-P-butyl blocks the formation of malonyl-CoA, disrupts lipid synthesis in sensitive plants, and exhibits concentration-dependent phytotoxicity to non-target maize seedlings. Fluazifop-P-butyl induces oxidative stress in male Wistar rats, impairs their liver and kidney functions, and disrupts testicular function.

Alisol A 24-acetate (Alisol A monoacetate) is an orally active derivative of protostane-type tetracyclic triterpenoid. Alisol A 24-acetate upregulates the expression of adiponectin, AMPKα, CPT1, and ACOX1; downregulates the expression of SREBP-1c, ACC, FAS, Bcl-2, Bcl-xl, PPAR-γ, perilipin A, and NFATc1; inhibits the activity of PI3K/Akt/mTOR and HMGR; and activates the PKA and ERK signaling pathways. Alisol A 24-acetate regulates cell apoptosis (apoptosis), autophagy (Autophagy, hepatic lipid accumulation, inflammatory response, neuroprotection, MRSA membrane integrity, and osteoclast differentiation. Alisol A 24-acetate can be used in research related to non-alcoholic fatty liver disease, nephrotoxicity, obesity, global cerebral ischemia-reperfusion injury, bacterial infection, and osteoporosis.

Sethoxydim is a postemergent herbicide. Sethoxydim inhibits plant acetyl-coenzyme A carboxylase (ACCase) activity.

hACC2-IN-1 is a potent acetyl-CoA carboxylase 2 (ACC2) inhibitor, with an IC₅₀ value of 2.5 μM (hACC2). hACC2-IN-1 could be used for obesity research.