Date published: 2026-4-1

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PKM2 Activators

PKM2 activators belong to a unique class of compounds that target the PKM2 (pyruvate kinase M2) enzyme. Pyruvate kinase is an essential enzyme in the glycolytic pathway, which is responsible for catalyzing the final step of glycolysis, converting phosphoenolpyruvate (PEP) to pyruvate. Among the different isoforms of pyruvate kinase found in mammals, PKM2 is unique in its ability to exist in both a dimeric and tetrameric form. The dimeric form of PKM2 is less active than the tetrameric form, leading to a bottleneck in the glycolytic pathway. This results in the accumulation of glycolytic intermediates that can be shunted into alternative pathways, such as the pentose phosphate pathway and serine biosynthesis, which are essential for the biosynthesis of nucleotides, amino acids, and lipids. PKM2 activators, as the name suggests, promote the formation of the active tetrameric form of PKM2, thereby enhancing its enzymatic activity. The interest in PKM2 activators stems from the observation that the dimeric form of PKM2 is often favored in rapidly proliferating cells, especially in certain tumor cells. The shift from the active tetrameric form to the less active dimeric form, known as the "PKM2 switch", allows these cells to balance their need for energy (in the form of ATP) with their need for biosynthetic precursors. By redirecting glycolytic intermediates into anabolic pathways, the PKM2 switch provides proliferating cells with the building blocks they need to grow and divide. PKM2 activators, by promoting the tetrameric form, can redirect cellular metabolism away from anabolic pathways and towards energy production. Understanding the molecular mechanisms by which PKM2 activators function and their effects on cellular metabolism is an active area of research, with the goal of uncovering new insights into metabolic regulation.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

D-Fructose 1,6-bisphosphate trisodium salt octahydrate

81028-91-3sc-221476
sc-221476A
1 g
5 g
$57.00
$97.00
1
(1)

D-Fructose 1,6-bisphosphate trisodium salt octahydrate serves as a crucial allosteric regulator in metabolic pathways, particularly in glycolysis. Its unique trisodium salt form enhances solubility, allowing for effective interaction with enzymes. The octahydrate structure provides a dynamic hydration environment, which stabilizes transient enzyme complexes. This compound's ability to modulate enzyme activity through specific molecular interactions underscores its role in cellular energy regulation and metabolic flux.

ML 265

1221186-53-3sc-492599
5 mg
$208.00
1
(0)

ML 265 is a selective activator of pyruvate kinase M2 (PKM2), influencing its dimer-tetramer equilibrium. This compound enhances PKM2's enzymatic activity by promoting its tetrameric form, which is crucial for efficient glycolytic flux. The unique binding interactions of ML 265 stabilize the enzyme's active conformation, facilitating substrate access and increasing reaction rates. Its distinct mechanism of action highlights the intricate regulation of metabolic pathways and energy homeostasis.

2-Deoxy-D-glucose

154-17-6sc-202010
sc-202010A
1 g
5 g
$70.00
$215.00
26
(2)

Inhibits glycolysis by targeting hexokinase. Cellular metabolic stress might indirectly affect PKM2 expression.

Sodium dichloroacetate

2156-56-1sc-203275
sc-203275A
10 g
50 g
$55.00
$209.00
6
(1)

Inhibits pyruvate dehydrogenase kinase (PDK), shifting metabolism from glycolysis to oxidative phosphorylation. This metabolic shift could potentially influence PKM2 levels.

1,1-Dimethylbiguanide, Hydrochloride

1115-70-4sc-202000F
sc-202000A
sc-202000B
sc-202000C
sc-202000D
sc-202000E
sc-202000
10 mg
5 g
10 g
50 g
100 g
250 g
1 g
$20.00
$43.00
$63.00
$156.00
$260.00
$510.00
$31.00
37
(1)

Activates AMP-activated protein kinase (AMPK) leading to decreased glycolysis. The metabolic reprogramming might indirectly upregulate PKM2.

Insulin

11061-68-0sc-29062
sc-29062A
sc-29062B
100 mg
1 g
10 g
$156.00
$1248.00
$12508.00
82
(1)

Stimulates glucose uptake and metabolism, potentially affecting PKM2 expression in certain contexts.

Cobalt(II) chloride

7646-79-9sc-252623
sc-252623A
5 g
100 g
$64.00
$176.00
7
(1)

Mimics hypoxic conditions by stabilizing HIF-1α, potentially promoting PKM2 expression under pseudo-hypoxic conditions.

Rapamycin

53123-88-9sc-3504
sc-3504A
sc-3504B
1 mg
5 mg
25 mg
$63.00
$158.00
$326.00
233
(4)

By inhibiting mTOR, Rapamycin affects cell growth and metabolism, which might indirectly influence PKM2 expression as part of metabolic reprogramming.

MK-2206 dihydrochloride

1032350-13-2sc-364537
sc-364537A
5 mg
10 mg
$182.00
$332.00
67
(1)

Akt signaling promotes glycolysis, so inhibiting Akt might cause metabolic shifts that could influence PKM2 levels.

Wortmannin

19545-26-7sc-3505
sc-3505A
sc-3505B
1 mg
5 mg
20 mg
$67.00
$223.00
$425.00
97
(3)

By inhibiting PI3K, Wortmannin affects downstream Akt and mTOR signaling, potentially influencing PKM2 expression due to shifts in cellular metabolism.