Synapsin Ia Inhibitors
Chemical inhibitors of Synapsin Ia play a crucial role in modulating its function by preventing phosphorylation, which is key to its role in neurotransmitter release. Phorbol 12-myristate 13-acetate, for instance, is an activator of protein kinase C (PKC), and its action leads to the phosphorylation and subsequent inhibition of Synapsin Ia's ability to bind to synaptic vesicles. This phosphorylation by PKC alters the dynamics of neurotransmitter release. Conversely, inhibitors like Bisindolylmaleimide I, Gö 6983, and Ro 31-8220 directly target PKC, thereby preventing the phosphorylation of Synapsin Ia. Staurosporine and its analog K252a, along with Balanol, are broad-spectrum kinase inhibitors that also inhibit PKC, resulting in reduced phosphorylation of Synapsin Ia and consequently its activity in vesicle trafficking.
Furthermore, Chelerythrine and Sphingosine are inhibitors that specifically target PKC, leading to decreased phosphorylation of Synapsin Ia. Ruboxistaurin, which selectively inhibits PKCβ, represents a more targeted approach, inhibiting the phosphorylation of Synapsin Ia by this specific kinase isoform. Lastly, Calphostin C binds to the regulatory domain of PKC in a light-dependent manner, offering a unique mechanism of inhibiting Synapsin Ia phosphorylation and its subsequent synaptic functions. Each of these chemical inhibitors contributes to the modulation of Synapsin Ia by impacting its phosphorylation state, which is crucial for its role in the regulation of neurotransmitter release from synaptic vesicles.
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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 | $40.00 $129.00 $210.00 $490.00 $929.00 | 119 | |
Phorbol esters like Phorbol 12-myristate 13-acetate activate protein kinase C (PKC) which can phosphorylate Synapsin Ia on specific sites leading to its functional inhibition. The phosphorylation by PKC alters Synapsin Ia's ability to bind synaptic vesicles and regulate their release. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
Bisindolylmaleimide I is a specific inhibitor of PKC, which is responsible for phosphorylating Synapsin Ia. By inhibiting PKC, Bisindolylmaleimide I prevents the phosphorylation of Synapsin Ia, therefore hindering its regulation of neurotransmitter release. | ||||||
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $150.00 $388.00 | 113 | |
Staurosporine is a potent inhibitor of many protein kinases, including PKC. By inhibiting PKC, Staurosporine can prevent the phosphorylation of Synapsin Ia, thereby inhibiting its function in synaptic vesicle trafficking and neurotransmitter release. | ||||||
Gö 6983 | 133053-19-7 | sc-203432 sc-203432A sc-203432B | 1 mg 5 mg 10 mg | $103.00 $293.00 $465.00 | 15 | |
Gö 6983 is a pan-PKC inhibitor that can prevent the phosphorylation of Synapsin Ia by inhibiting PKC activity. This blockage of PKC-mediated phosphorylation inhibits the function of Synapsin Ia in the regulation of neurotransmitter release. | ||||||
K-252a | 99533-80-9 | sc-200517 sc-200517B sc-200517A | 100 µg 500 µg 1 mg | $126.00 $210.00 $488.00 | 19 | |
K252a, a staurosporine analogue, serves as an inhibitor for a broad range of protein kinases. By inhibiting these kinases, K252a can decrease the phosphorylation of Synapsin Ia thereby inhibiting its role in the modulation of neurotransmitter release. | ||||||
Ro 31-8220 | 138489-18-6 | sc-200619 sc-200619A | 1 mg 5 mg | $90.00 $240.00 | 17 | |
Ro 31-8220 is an inhibitor of PKC, and therefore can inhibit the phosphorylation of Synapsin Ia which is necessary for its role in the regulation of neurotransmitter release at synapses. | ||||||
Chelerythrine | 34316-15-9 | sc-507380 | 100 mg | $540.00 | ||
Chelerythrine is known to inhibit PKC, which is responsible for phosphorylating Synapsin Ia. The inhibition of PKC by Chelerythrine would lead to a decrease in Synapsin Ia phosphorylation, and thus inhibit its function in neurotransmitter release. | ||||||
Ruboxistaurin | 169939-94-0 | sc-507364 | 25 mg | $1080.00 | ||
Ruboxistaurin selectively inhibits PKCβ, which is one of the isoforms of PKC that can phosphorylate Synapsin Ia. By inhibiting this isoform, Ruboxistaurin can decrease the phosphorylation and therefore inhibit the function of Synapsin Ia in synaptic vesicle dynamics. | ||||||
Balanol | 63590-19-2 | sc-503251 | 10 mg | $13500.00 | ||
Balanol is an analog of staurosporine and acts as an inhibitor of protein kinase C. By inhibiting PKC, it would prevent the phosphorylation of Synapsin Ia, thereby inhibiting its role in the regulation of neurotransmitter release. | ||||||
D-erythro-Sphingosine | 123-78-4 | sc-3546 sc-3546A sc-3546B sc-3546C sc-3546D sc-3546E | 10 mg 25 mg 100 mg 1 g 5 g 10 g | $88.00 $190.00 $500.00 $2400.00 $9200.00 $15000.00 | 2 | |
Sphingosine acts as an inhibitor of protein kinase C. By inhibiting PKC, Sphingosine can prevent the phosphorylation of Synapsin Ia, which is required for its function in vesicle trafficking and neurotransmitter release. | ||||||