Date published: 2026-5-6

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Calpain 3 Inhibitors

Calpain 3 inhibitors encompass a range of chemicals that, while not directly interacting with the protease, induce a decrease in its activity through the modulation of cellular calcium levels. The activity of Calpain 3 is intimately linked with calcium homeostasis, and the compounds listed serve to disturb this balance, leading to a reduction in Calpain 3 proteolytic activity. These compounds employ different mechanisms to achieve this effect. Some act at the level of calcium channels, either blocking the channels themselves or the receptors that control the channels, thereby decreasing calcium influx. Others chelate calcium directly within the cell or affect the storage and release mechanisms that supply calcium for Calpain 3 activation. This group of inhibitors includes calcium channel blockers such as verapamil, nifedipine, and amlodipine, which are traditionally used for cardiovascular indications but have a secondary function in controlling cellular calcium levels. The inhibition of calcium signaling pathways represents a crucial strategy in modulating Calpain 3 activity. Calpain 3's role in myopathies underscores the importance of precise calcium regulation within muscle cells, and these compounds have the capacity to alter the delicate balance of calcium ions necessary for Calpain 3 function. The action of these inhibitors is further distinguished by their specific targets, whether they be the voltage-gated L-type calcium channels, which are crucial for excitation-contraction coupling in muscle cells, or the intracellular calcium stores that supply the necessary ions for a multitude of cellular processes including enzymatic activation. By binding to various components of the calcium signaling machinery, these compounds reduce the amount of free calcium, leading to an indirect inhibition of Calpain 3. In essence, the effective reduction of Calpain 3 activity by these compounds is a consequence of their impact on calcium dynamics within cells.

Items 1 to 10 of 12 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Dantrolene

7261-97-4sc-500165
25 mg
$350.00
7
(0)

Dantrolene interferes with calcium release from the sarcoplasmic reticulum by antagonizing ryanodine receptors. By reducing intracellular calcium concentration, dantrolene can indirectly inhibit Calpain 3, which requires calcium for its enzymatic activity, leading to reduced proteolysis associated with this protease.

BAPTA/AM

126150-97-8sc-202488
sc-202488A
25 mg
100 mg
$138.00
$458.00
61
(2)

BAPTA-AM is a cell-permeable calcium chelator that upon hydrolysis by intracellular esterases binds calcium ions, thereby decreasing cytosolic calcium levels. As a result, it indirectly inhibits Calpain 3 activity by limiting the calcium availability necessary for its activation.

Omeprazole

73590-58-6sc-202265
50 mg
$67.00
4
(1)

Omeprazole, commonly known for its use as a proton pump inhibitor, can also raise the pH of intracellular compartments and influence calcium sequestration. This alteration in calcium handling can indirectly reduce Calpain 3 activation, as the protease is dependent on calcium ions.

Verapamil

52-53-9sc-507373
1 g
$374.00
(0)

Verapamil is a calcium channel blocker that impedes the influx of calcium through the L-type calcium channels. By reducing calcium availability in the muscle cells, verapamil can decrease the activation of Calpain 3, thereby indirectly inhibiting its proteolytic activity.

Gabapentin

60142-96-3sc-201481
sc-201481A
sc-201481B
20 mg
100 mg
1 g
$53.00
$94.00
$135.00
7
(1)

Gabapentin binds to the alpha-2-delta subunit of voltage-gated calcium channels, modulating calcium influx and potentially affecting downstream signaling pathways that can regulate protease activity, including Calpain 3, by limiting available calcium required for its function.

2-APB

524-95-8sc-201487
sc-201487A
20 mg
100 mg
$28.00
$53.00
37
(1)

2-APB acts as an inhibitor of IP3 receptors and store-operated calcium entry, affecting the calcium homeostasis within cells. By modulating calcium signaling, 2-APB can indirectly lead to the inhibition of Calpain 3 activity due to decreased levels of calcium which is crucial for the protease's activity.

SK&F 96365

130495-35-1sc-201475
sc-201475B
sc-201475A
sc-201475C
5 mg
10 mg
25 mg
50 mg
$103.00
$158.00
$397.00
$656.00
2
(1)

SKF-96365 inhibits receptor-mediated calcium entry and store-operated calcium channels, disrupting the calcium homeostasis in cells. The decrease in intracellular calcium levels can, therefore, indirectly inhibit Calpain 3 by reducing the calcium-dependent proteolytic processing that Calpain 3 mediates.

Bepridil

64706-54-3sc-507400
100 mg
$1620.00
(0)

Bepridil is a calcium channel blocker that decreases intracellular calcium levels by inhibiting both voltage-gated calcium channels and the release of calcium from intracellular stores. This reduction in calcium levels can indirectly inhibit the activity of calcium-dependent enzymes such as Calpain 3.

Flunarizine

52468-60-7sc-337841
5 g
$560.00
(0)

Flunarizine is a selective calcium entry blocker with calmodulin-binding properties and histamine H1 blocking activity. This compound's action reduces the cytosolic calcium levels, indirectly inhibiting Calpain 3 activity by diminishing the calcium ion concentration necessary for the proteases activity.

TMB-8 • HCl

53464-72-5sc-3522
sc-3522A
10 mg
50 mg
$43.00
$129.00
10
(1)

TMB-8 (Trifluoperazine) is known to inhibit intracellular calcium release, impacting the function of enzymes that are dependent on calcium ions, such as Calpain 3. By reducing the availability of calcium, TMB-8 can indirectly inhibit the enzymatic activity of Calpain 3.