Biological Information

Background Information:

Acetyl-CoA carboxylase 2 (ACC2), also known as ACC-beta, is a biotin-dependent enzyme that catalyzes the conversion of acetyl-CoA to malonyl-CoA, a key step in fatty acid metabolism. As one of two ACC isoforms, ACC2 is primarily expressed in oxidative tissues such as the heart, skeletal muscle, and liver, where it localizes to mitochondria. It regulates fatty acid β-oxidation by producing malonyl-CoA, which inhibits carnitine palmitoyltransferase I (CPT1), the rate-limiting enzyme for mitochondrial fatty acid uptake. This inhibition reduces fatty acid oxidation and helps balance lipid storage and utilization. ACC2 is inhibited by AMP-activated protein kinase (AMPK) during energy stress. Dysregulation of ACC2 contributes to metabolic disorders, including obesity, type 2 diabetes, fatty liver, and cardiovascular disease. Its pivotal role in lipid balance and energy regulation makes ACC2 a compelling therapeutic target for metabolic disease intervention.

Family:

Lipid Metabolism

Class:

Lipid metabolism

Accession Number:

NM_001093

Organism:

Human

Construct Details:

Full length, Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Luminescence

Measured Response:

Luminescence

Testing Information

Procedure Summary:

Human recombinant ACC2 enzyme expressed in Sf9 cells is used. Test compound and/or vehicle is preincubated with 0.50 μg/ml active enzyme in modified HEPES buffer pH 7.4 for 15 minutes at 25oC. The reaction is initiated by addition of 20 µM Acetyl-CoA for another 30 minutes incubation period. Determination of the amount of ADP formed by ADP-Glo™ Kinase Assay Kit is read luminescence on a spectrophotometer. Compounds are screened at 10 μM.

Substrate:

20 µM Acetyl-CoA

Incubation:

30 min at 25°C

Control Inhibitor:

Firsocostat

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

Test Sample Requirements:

Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).

Minimum Order Quantity:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

11681998

Name

A-908292

Measurement

0.27μM - IC50

PubChem ID

71528744

Name

Firsocostat

Measurement

0.0091μM - IC50

PubChem ID

52934180

Name

PF-05175157

Measurement

0.079μM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei