Date published: 2026-5-4

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PEPCK-M Inhibitors

Common PEPCK-M Inhibitors include, but are not limited to 3-Mercaptopicolinic Acid, Hydrochloride CAS 320386-54-7, α-Ketoglutaric Acid CAS 328-50-7, 3-Methyl-2-oxovaleric Acid CAS 1460-34-0, 5-Benzimidazolecarboxylic acid CAS 15788-16-6 and trans-Cinnamamide CAS 22031-64-7.

PEPCK-M inhibitors belong to a distinct chemical class that specifically targets and modulates the activity of the mitochondrial isoform of phosphoenolpyruvate carboxykinase (PEPCK-M). This enzyme plays a crucial role in the regulation of glucose metabolism and gluconeogenesis. PEPCK-M primarily functions within the mitochondria of liver cells, where it catalyzes the conversion of oxaloacetate to phosphoenolpyruvate, a critical step in gluconeogenesis – the process by which glucose is synthesized from non-carbohydrate precursors.

By inhibiting the activity of PEPCK-M, these compounds impact the rate of glucose production in the liver. This can have broad implications for glucose homeostasis and energy metabolism, as gluconeogenesis is an essential process that maintains blood glucose levels during periods of fasting and nutrient scarcity. Investigating the effects of PEPCK-M inhibitors sheds light on the intricate molecular mechanisms underlying glucose regulation, cellular energy balance, and the intricate interplay between different metabolic pathways. Understanding these mechanisms offers insights into metabolic disorders, diabetes, and other conditions linked to aberrant glucose metabolism. This exploration contributes to our comprehension of the complex network of metabolic reactions that govern overall physiological function.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

3-Mercaptopicolinic Acid, Hydrochloride

320386-54-7sc-206655
1 g
$302.00
7
(1)

3-Mercaptopicolinic acid is a structural analog of phosphoenolpyruvate (PEP) and is thought to inhibit PEPCK-M by competitively binding to its active site. By doing so, it interferes with the catalytic activity of PEPCK-M, leading to reduced conversion of oxaloacetate to PEP and impairing gluconeogenesis.

α-Ketoglutaric Acid

328-50-7sc-208504
sc-208504A
sc-208504B
sc-208504C
sc-208504D
sc-208504E
sc-208504F
25 g
100 g
250 g
500 g
1 kg
5 kg
16 kg
$33.00
$43.00
$63.00
$110.00
$188.00
$738.00
$2091.00
2
(1)

α-Ketoglutaric Acid is an α-ketoglutarate analog that might act as a competitive inhibitor of PEPCK-M. Its structural similarity to oxaloacetate allows it to bind to the active site of PEPCK-M, potentially interfering with its catalytic activity and reducing the production of phosphoenolpyruvate, a key step in gluconeogenesis.

3-Methyl-2-oxovaleric Acid

1460-34-0sc-484817
1 g
$326.00
(1)

This compound is an α-keto acid analog that could potentially inhibit PEPCK-M by binding to its active site, similar to the natural substrate phosphoenolpyruvate (PEP). By competing with PEP for binding, it might hinder the catalytic conversion of oxaloacetate to PEP, ultimately impacting gluconeogenesis.

5-Benzimidazolecarboxylic acid

15788-16-6sc-226912
5 g
$50.00
(0)

Although specific information on this compound is limited, benzimidazole-5-carboxylic acid might act as an inhibitor of PEPCK-M. Its mechanism could involve binding to the enzyme's active site or allosteric sites, affecting its catalytic activity and reducing gluconeogenic flux.

trans-Cinnamamide

22031-64-7sc-296584
25 g
$238.00
(0)

Similar to benzoic acid derivatives, cinnamic acid derivatives might exert inhibitory effects on PEPCK-M through diverse mechanisms, including active site binding or allosteric modulation, ultimately leading to decreased phosphoenolpyruvate production and gluconeogenesis.

Aspirin

50-78-2sc-202471
sc-202471A
5 g
50 g
$20.00
$42.00
4
(1)

Aspirin, a well-known anti-inflammatory drug, might have inhibitory effects on PEPCK-M. Its mechanism could involve modulating the enzyme's activity indirectly through its impact on cellular signaling pathways, metabolism, or energy balance, which could influence gluconeogenesis.

3-Guanidinopropionic acid

353-09-3sc-254485
sc-254485A
1 g
5 g
$56.00
$197.00
(1)

Guanidinopropionic acid is a guanidine analog that could potentially influence PEPCK-M activity. Its mechanism might involve competing with or binding to PEP or its binding sites, potentially impairing the enzyme's catalytic function and decreasing gluconeogenesis.

2-(acetylamino)-3-mercapto-3-methylbutanoic acid

59-53-0sc-340087
sc-340087A
1 g
5 g
$312.00
$915.00
(0)

This compound, a mercapto analog, could potentially inhibit PEPCK-M through mechanisms similar to other mercapto compounds. Its structural resemblance to PEP might allow it to bind to the enzyme's active site, interfering with its catalytic activity and reducing gluconeogenic output.

D,L-threo-β-Hydroxyaspartic acid

4294-45-5sc-207500A
sc-207500
sc-207500B
50 mg
100 mg
1 g
$235.00
$286.00
$2040.00
(0)

Although specific information is limited, β-hydroxyaspartic acid could potentially impact PEPCK-M. Its mechanism might involve competitive or allosteric interactions with the enzyme, leading to changes in its catalytic activity and affecting gluconeogenesis.