Date published: 2026-2-23

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Calpain 3 Activators

Calpain 3 activators represent a category of chemicals that enhance the activity of Calpain 3 primarily through the elevation of intracellular calcium levels, which is a crucial activator for the protease. These chemicals achieve this by either directly introducing calcium into the cellular environment or by manipulating the pathways and channels that govern calcium influx and storage. Some compounds, like Ionophycin, function as ionophores that directly transport calcium ions into the cell, effectively bypassing the cellular control mechanisms of calcium entry. Others, such as the enantiomers of Bay K 8644, operate by activating the L-type calcium channels, thereby promoting an increased calcium influx, which directly correlates with the activation state of Calpain 3.Within the group, certain activators work by disrupting the calcium sequestration in the endoplasmic and sarcoplasmic reticulum. Thapsigargin and Cyclopiazonic acid are two such examples that, by inhibiting the SERCA pump, lead to a sustained increase in cytosolic calcium concentration. Other compounds like HG-9-91-01 function indirectly by influencing phosphatases that are upstream regulators of signaling pathways affecting calcium dynamics. This, in turn, causes an accumulation of cytosolic calcium, leading to the activation of Calpain 3. Additionally, modulators of cellular action potentials like 4-aminopyridine, by prolonging the action potential duration, facilitate greater calcium entry during neuronal firing. Collectively, these activators engage with different components of the calcium handling and signaling machinery of the cell, resulting in a common outcomeenhanced Calpain 3 activity due to increased availability of calcium.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Ionomycin, free acid

56092-81-0sc-263405
sc-263405A
1 mg
5 mg
$96.00
$264.00
2
(2)

Ionophore that specifically binds and transports calcium ions across membranes, raising intracellular calcium levels. This elevation in calcium directly activates Calpain 3 by providing the necessary ions for its enzymatic function.

BAY K 8644, S(−)-

98625-26-4sc-203525
sc-203525A
10 mg
50 mg
$398.00
$1428.00
1
(1)

A dihydropyridine that acts as an L-type calcium channel agonist, promoting the influx of calcium into the cell. Increased intracellular calcium levels subsequently activate Calpain 3 by satisfying its calcium requirement for activation.

4-Aminopyridine

504-24-5sc-202421
sc-202421B
sc-202421A
25 g
1 kg
100 g
$38.00
$1155.00
$122.00
3
(2)

Blocks voltage-gated potassium channels, which prolongs action potentials and enhances calcium entry into neurons through voltage-dependent calcium channels, thereby increasing the intracellular calcium concentration and indirectly activating Calpain 3.

Thapsigargin

67526-95-8sc-24017
sc-24017A
1 mg
5 mg
$136.00
$446.00
114
(2)

A sesquiterpene lactone that inhibits the sarcoplasmic/endoplasmic reticulum Ca2+-ATPase (SERCA), leading to an increase in cytosolic calcium concentration and thereby indirectly activates Calpain 3.

Pimozide

2062-78-4sc-203662
100 mg
$104.00
3
(1)

Blocks dopamine receptors, which leads to alterations in intracellular signaling pathways, including those regulating calcium homeostasis. This can result in increased calcium levels, thereby activating Calpain 3.

FPL-64176

120934-96-5sc-201491
5 mg
$83.00
1
(1)

Selective L-type calcium channel activator which increases calcium influx into the cell, thus indirectly activating Calpain 3 by providing higher intracellular calcium necessary for its activity.

Aristolochic Acid

313-67-7sc-200731
25 mg
$96.00
2
(2)

Inhibits nitric oxide synthase, which can lead to an increase in intracellular calcium concentrations and thereby indirectly activate Calpain 3.

Cyclopiazonic Acid

18172-33-3sc-201510
sc-201510A
10 mg
50 mg
$176.00
$624.00
3
(1)

Inhibits the SERCA, causing an increase in cytosolic calcium levels that in turn activates Calpain 3.

A23187

52665-69-7sc-3591
sc-3591B
sc-3591A
sc-3591C
1 mg
5 mg
10 mg
25 mg
$55.00
$131.00
$203.00
$317.00
23
(1)

A calcium ionophore that increases intracellular calcium concentration by transporting calcium across the cell membrane, which directly activates Calpain 3.