CaMKIIγ Inhibitors
The class of compounds referred to as CaMKIIγ inhibitors encompasses diverse chemical entities that directly or indirectly modulate the activity of CaMKIIγ, a calcium/calmodulin-dependent protein kinase with essential roles in neuronal function. KN-93 and KN-62 directly interfere with CaMKIIγ by disrupting the Ca2+/calmodulin-dependent activation, while AIP, a synthetic peptide, competes with ATP binding, preventing CaMKIIγ activation. Additionally, compounds like Compound 48/80 and Calmidazolium chloride indirectly impact CaMKIIγ by affecting histamine release and calmodulin binding, respectively.
Notably, the irreversible photoaffinity label N-(4-Azido-2-nitrophenyl) modifies CaMKIIγ structure, inhibiting its activity. SD-208, originally a TGF-β signaling inhibitor, indirectly modulates CaMKIIγ through pathway crosstalk. Compound 19, an inhibitor of PP2A, alters CaMKIIγ phosphorylation status, influencing its activity. Peptide inhibitor TAT-CN21 blocks CaMKIIγ activation by interfering with autoregulation, and Calmodulin Antagonist W-7 disrupts Ca2+/calmodulin binding to inhibit CaMKIIγ. Furthermore, A-484954, a TRPV1 inhibitor, indirectly modulates CaMKIIγ by affecting calcium influx, influencing downstream signaling pathways.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
KN-93 | 139298-40-1 | sc-202199 | 1 mg | $178.00 | 25 | |
KN-93 is a specific inhibitor of CaMKII, affecting both CaMKIIα and CaMKIIβ isoforms. Its inhibitory action on CaMKIIγ is inferred based on the structural similarities among CaMKII isoforms. KN-93 exerts its inhibitory effect by interfering with Ca2+/calmodulin binding to the kinase, preventing its activation. This disruption impedes CaMKIIγ-dependent signaling cascades, thereby indirectly inhibiting the activity of CaMKIIγ. | ||||||
KN-62 | 127191-97-3 | sc-3560 | 1 mg | $133.00 | 20 | |
KN-62 is a broad-spectrum CaMK inhibitor, targeting CaMKI, CaMKII, and CaMKIV. Its inhibition of CaMKII has implications for CaMKIIγ function. KN-62 interferes with the Ca2+/calmodulin-dependent activation of CaMKII, leading to a blockade of downstream signaling events involving CaMKIIγ. By disrupting the activation of CaMKII, KN-62 indirectly influences cellular processes regulated by CaMKIIγ, such as synaptic plasticity and calcium signaling. | ||||||
Aluminum isopropoxide | 555-31-7 | sc-239217 | 100 g | $37.00 | ||
Autocamtide-2-related inhibitory peptide (AIP) is a synthetic peptide designed to selectively inhibit CaMKII by competing with its substrate ATP. While AIP has been primarily used for CaMKIIα, its inhibitory mechanism can extend to other CaMKII isoforms, including CaMKIIγ. By preventing ATP binding to the kinase, AIP disrupts the phosphorylation events orchestrated by CaMKII, leading to indirect modulation of CaMKIIγ-dependent cellular processes. | ||||||
Compound 48/80 trihydrochloride | 94724-12-6 | sc-200736 sc-200736A sc-200736B sc-200736C | 100 mg 250 mg 1 g 5 g | $102.00 $214.00 $826.00 $3682.00 | ||
Compound 48/80 is a mast cell degranulator that indirectly affects CaMKIIγ through its impact on histamine release. Histamine, a CaMKIIγ regulator, can activate CaMKIIγ by binding to its regulatory domain. Compound 48/80 induces histamine release, leading to increased CaMKIIγ activity. This indirect modulation influences cellular processes where CaMKIIγ plays a role, such as neurotransmitter release and calcium homeostasis. | ||||||
Calmidazolium chloride | 57265-65-3 | sc-201494 sc-201494A | 10 mg 50 mg | $153.00 $600.00 | 27 | |
Calmidazolium chloride is a calmodulin antagonist that indirectly inhibits CaMKIIγ by interfering with the Ca2+/calmodulin complex formation. As CaMKIIγ activation relies on calmodulin binding, calmidazolium chloride disrupts this interaction, preventing the activation of CaMKIIγ. The subsequent inhibition of CaMKIIγ-mediated signaling pathways results from the disruption of the normal regulatory mechanisms governing CaMKIIγ activation. | ||||||
TGF-β RI Kinase Inhibitor V | 627536-09-8 | sc-203294 | 2 mg | $86.00 | 3 | |
SD-208 is a potent and selective inhibitor of TGF-β type I receptor kinase (ALK5), affecting TGF-β signaling pathways. Although not a direct inhibitor of CaMKIIγ, SD-208 indirectly modulates CaMKIIγ-dependent processes by interfering with TGF-β signaling cascades. TGF-β pathways are known to intersect with CaMKIIγ signaling in certain cellular contexts, and SD-208's impact on these pathways influences CaMKIIγ-dependent functions, such as synaptic plasticity and neuronal excitation. | ||||||
W-7 | 61714-27-0 | sc-201501 sc-201501A sc-201501B | 50 mg 100 mg 1 g | $163.00 $300.00 $1642.00 | 18 | |
Calmodulin Antagonist W-7 is a calmodulin antagonist that indirectly inhibits CaMKIIγ by interfering with the Ca2+/calmodulin complex formation. As CaMKIIγ activation relies on calmodulin binding, W-7 disrupts this interaction, preventing the activation of CaMKIIγ. The subsequent inhibition of CaMKIIγ-mediated signaling pathways, including those involved in neuronal plasticity, results from the disruption of the normal regulatory mechanisms governing CaMKIIγ activation. | ||||||
A 484954 | 142557-61-7 | sc-479613 | 10 mg | $175.00 | ||
A-484954 is a selective inhibitor of the transient receptor potential cation channel subfamily V member 1 (TRPV1). It indirectly modulates CaMKIIγ by affecting calcium influx through TRPV1 channels. The inhibition of TRPV1 by A-484954 reduces calcium-dependent activation of CaMKIIγ, impacting downstream signaling pathways regulated by CaMKIIγ. This indirect modulation influences cellular processes such as synaptic plasticity and neuronal excitation, where CaMKIIγ plays a crucial role. | ||||||