Munc13-1 Activators
Munc13-1 activators are compounds that indirectly or directly enhance the functional activity of Munc13-1, a crucial protein in synaptic vesicle priming and neurotransmitter release. The activity of Munc13-1 is significantly regulated by phosphorylation events, primarily mediated by protein kinase C (PKC). Compounds such as Phorbol 12-myristate 13-acetate (PMA) and Diacylglycerol (DAG) activate PKC, which then phosphorylates Munc13-1, enhancing its vesicle priming activity. Similarly, 1-Oleoyl-2-acetyl-sn-glycerol (OAG), a synthetic analog of DAG, serves to activate PKC, leading to increased Munc13-1 activity. Furthermore, the modulation of membrane fluidity by compounds such as Docosahexaenoic acid (DHA) can affect Munc13-1's interactions at the synaptic membrane, thereby influencing its function in vesicle fusion.
Other compounds such as calcium ionophores exemplified by A23187, raise intracellular calcium levels, which in turn enhance the calcium-dependent activation of Munc13-1. Additionally, Farnesyltransferase inhibitors (FTIs) may indirectly result in the enhanced activity of Munc13-1 by altering the prenylation-dependent membrane association of proteins that regulate the localization and function of Munc13-1. Epigallocatechin gallate (EGCG) and Ginkgolide B modulate lipid signaling pathways, which can indirectly enhance the activity of Munc13-1 in synaptic vesicle priming. Genistein, through its kinase inhibition, can lead to compensatory cellular signaling mechanisms that enhance Munc13-1 function, and Ryanodine, by modulating intracellular calcium release, can also enhance the activity of Munc13-1.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
PMA | 16561-29-8 | sc-3576 sc-3576A sc-3576B sc-3576C sc-3576D | 1 mg 5 mg 10 mg 25 mg 100 mg | $41.00 $132.00 $214.00 $500.00 $948.00 | 119 | |
PMA is a potent activator of protein kinase C (PKC), which can phosphorylate Munc13-1. The phosphorylation of Munc13-1 by PKC is known to enhance its activity in vesicle priming, a critical step in synaptic transmission. | ||||||
R 59-022 | 93076-89-2 | sc-203227 | 5 mg | $124.00 | 1 | |
DAG functions as a second messenger that activates PKC. The activation of PKC can subsequently enhance the phosphorylation and activity of Munc13-1 in the regulation of neurotransmitter release at synapses. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $105.00 $242.00 | 36 | |
BIM-1 is a selective inhibitor of PKC isoforms. While an inhibitor, it can lead to a compensatory increase in DAG levels to maintain PKC activity, indirectly enhancing Munc13-1 function through increased PKC-mediated phosphorylation in a feedback mechanism. | ||||||
Docosahexaenoic Acid N-Succinimide | 160801-26-3 | sc-496899 | 25 mg | $317.00 | ||
DHA can modulate membrane fluidity and microdomain formation, which may affect the localization and function of Munc13-1 at synaptic terminals, as Munc13-1 is known to interact with specific lipid environments for its proper functioning in vesicle fusion. | ||||||
A23187 | 52665-69-7 | sc-3591 sc-3591B sc-3591A sc-3591C | 1 mg 5 mg 10 mg 25 mg | $55.00 $131.00 $203.00 $317.00 | 23 | |
A23187 increases intracellular calcium levels, which can enhance the calcium-dependent activation of Munc13-1, crucial for its role in synaptic vesicle priming and neurotransmitter release. | ||||||
1-Oleoyl-2-acetyl-sn-glycerol (OAG) | 86390-77-4 | sc-200417 sc-200417A | 10 mg 50 mg | $119.00 $453.00 | 1 | |
OAG is a synthetic analog of DAG and can activate PKC, leading to the enhanced phosphorylation and subsequent activity of Munc13-1 in synaptic vesicle priming. | ||||||
(−)-Epigallocatechin Gallate | 989-51-5 | sc-200802 sc-200802A sc-200802B sc-200802C sc-200802D sc-200802E | 10 mg 50 mg 100 mg 500 mg 1 g 10 g | $43.00 $73.00 $126.00 $243.00 $530.00 $1259.00 | 11 | |
EGCG can modulate lipid signaling pathways, potentially altering the interaction of Munc13-1 with membrane lipids and enhancing its membrane binding and activity in neurotransmitter release. | ||||||
Ginkgolide B | 15291-77-7 | sc-201037B sc-201037 sc-201037C sc-201037A | 5 mg 10 mg 25 mg 50 mg | $46.00 $64.00 $114.00 $201.00 | 8 | |
Ginkgolide B is known to influence synaptic function and plasticity. It may indirectly enhance Munc13-1 activity by modulating the lipid environment and signaling pathways that Munc13-1 is involved in, thus facilitating vesicle priming and neurotransmitter release. | ||||||
Genistein | 446-72-0 | sc-3515 sc-3515A sc-3515B sc-3515C sc-3515D sc-3515E sc-3515F | 100 mg 500 mg 1 g 5 g 10 g 25 g 100 g | $45.00 $164.00 $200.00 $402.00 $575.00 $981.00 $2031.00 | 46 | |
Genistein is a tyrosine kinase inhibitor that, by inhibiting certain kinases, could lead to an upregulation of Munc13-1 activity due to compensatory cellular signaling mechanisms aiming to maintain synaptic transmission efficacy. | ||||||
Ryanodine | 15662-33-6 | sc-201523 sc-201523A | 1 mg 5 mg | $223.00 $799.00 | 19 | |
Ryanodine modulates the release of calcium from intracellular stores, potentially increasing the calcium-dependent activity of Munc13-1, which is essential for its role in synaptic vesicle priming. | ||||||