MCTP2 Inhibitors
MCTP2 inhibitors encompass a diverse range of chemical compounds that target the calcium-dependent aspects of MCTP2's functions in membrane trafficking. For instance, BAPTA-AM and Thapsigargin both act to perturb the intracellular calcium balance, which is crucial for MCTP2's activity; BAPTA-AM achieves this through selective chelation of calcium, while Thapsigargin disrupts the ER calcium stores by inhibiting the SERCA pump. Similarly, 2-APB and Xestospongin C target the IP3 receptor-mediated calcium release, and SKF-96365 inhibits receptor-mediated calcium entry channels, all crucial in maintaining the calcium signaling upon which MCTP2 depends. Compounds like ML-9 and U-73122 indirectly hinder MCTP2 activity by their action on upstream kinases and enzymes, MLCK and phospholipase C, respectively, which are involved in the regulation of cytoskeletal dynamics and secondary messenger production critical for MCTP2-mediated processes.
Further inhibitory effects on MCTP2 are achieved through modulation of calcium influx and release by compounds such as Nifedipine, TMB-8, Ryanodine, and KN-93. Nifedipine, an L-type calcium channel blocker, limits calcium influx, thus indirectly diminishing MCTP2's activity. TMB-8 and Ryanodine interfere with calcium release from internal stores, with TMB-8 acting as an inhibitor and Ryanodine causing depletion by locking the ryanodine receptor in an open state. Additionally, W-7 and KN-93 serve as antagonists to proteins that interact with calcium to modulate MCTP2 function: W-7 inhibits calmodulin-dependent processes, and KN-93 targets CaMKII, a kinase that phosphorylates proteins involved in calcium signaling pathways. Collectively, these inhibitors utilize different molecular mechanisms to reduce the functional activity of MCTP2, highlighting the integral role of calcium in the regulation of this protein's trafficking capabilities.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
BAPTA/AM | 126150-97-8 | sc-202488 sc-202488A | 25 mg 100 mg | $138.00 $458.00 | 61 | |
BAPTA-AM is a selective calcium chelator that can decrease intracellular calcium levels. MCTP2 is a calcium-dependent membrane trafficking protein, and by chelating calcium, BAPTA-AM inhibits the calcium-dependent functions of MCTP2, leading to a reduction in its activity. | ||||||
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $136.00 $446.00 | 114 | |
Thapsigargin is a SERCA pump inhibitor that leads to the depletion of intracellular calcium stores. By disrupting calcium homeostasis, thapsigargin indirectly affects MCTP2 activity, which relies on calcium for its trafficking functions. | ||||||
2-APB | 524-95-8 | sc-201487 sc-201487A | 20 mg 100 mg | $28.00 $53.00 | 37 | |
2-APB is an inhibitor of IP3 receptors and store-operated calcium channels. By inhibiting these channels, 2-APB reduces calcium signaling, which is necessary for MCTP2-mediated membrane trafficking. | ||||||
Xestospongin C | 88903-69-9 | sc-201505 | 50 µg | $510.00 | 14 | |
Xestospongin C is a potent inhibitor of IP3 receptors. It prevents the release of calcium from the endoplasmic reticulum, thus interfering with calcium-dependent processes in which MCTP2 is involved. | ||||||
SK&F 96365 | 130495-35-1 | sc-201475 sc-201475B sc-201475A sc-201475C | 5 mg 10 mg 25 mg 50 mg | $103.00 $158.00 $397.00 $656.00 | 2 | |
SKF-96365 is an inhibitor of receptor-mediated calcium entry channels. By inhibiting these channels, it disrupts calcium signaling pathways that MCTP2 requires to function effectively. | ||||||
ML-9 | 105637-50-1 | sc-200519 sc-200519A sc-200519B sc-200519C | 10 mg 50 mg 100 mg 250 mg | $112.00 $449.00 $673.00 $1224.00 | 2 | |
ML-9 is a kinase inhibitor that can inhibit myosin light-chain kinase (MLCK). Since MLCK is involved in cytoskeletal rearrangements that are part of membrane trafficking, its inhibition by ML-9 can indirectly reduce MCTP2 activity. | ||||||
Ryanodine | 15662-33-6 | sc-201523 sc-201523A | 1 mg 5 mg | $223.00 $799.00 | 19 | |
Ryanodine locks the ryanodine receptor in an open state, depleting calcium stores and disrupting calcium signaling. The disrupted signaling indirectly affects MCTP2's function in membrane trafficking. | ||||||
Nifedipine | 21829-25-4 | sc-3589 sc-3589A | 1 g 5 g | $59.00 $173.00 | 15 | |
Nifedipine is an L-type calcium channel blocker. By blocking these channels, it diminishes calcium influx thereby indirectly inhibiting MCTP2 activity which is dependent on calcium. | ||||||
TMB-8 • HCl | 53464-72-5 | sc-3522 sc-3522A | 10 mg 50 mg | $43.00 $129.00 | 10 | |
TMB-8 is an inhibitor of intracellular calcium release. It works by blocking the release of calcium from internal stores, indirectly affecting the calcium-dependent functions of MCTP2. | ||||||
W-7 | 61714-27-0 | sc-201501 sc-201501A sc-201501B | 50 mg 100 mg 1 g | $166.00 $306.00 $1675.00 | 18 | |
W-7 is a calmodulin antagonist which interferes with calcium-calmodulin-dependent processes. Since MCTP2 activity is calcium-dependent, W-7 can indirectly inhibit its function. | ||||||