Dynamin inhibitory peptide

Dynamin Inhibitory Peptide is a peptide inhibitor of the GTPase dynamin, which competitively blocks binding of dynamin to amphiphysin, thus it prevents endocytosis when administered intracellularly. It lead to GABAA receptor internalization reduce and miniature ISPC amplitude and frequency in neurons expressing GABAA receptors increase.

Designed for biological research and industrial applications, not intended for individual clinical or medical purposes.
Dynamin inhibitory peptide(CAS 251634-21-6)

CAT No: R0850

CAS No:251634-21-6

Synonyms/Alias:Dynamin inhibitory peptide;251634-21-6;L-Proline, L-glutaminyl-L-valyl-L-prolyl-L-seryl-L-arginyl-L-prolyl-L-asparaginyl-L-arginyl-L-alanyl-;QVPSRPNRAP;HY-P1083;AKOS024456770;DA-63063;MS-31983;CS-0027626;G13347;

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cGMP Peptide
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  • IND and NDA support
  • Drug master files (DMF) filing
M.F/Formula
C47H80N18O14
M.W/Mr.
1121.3
Sequence
One Letter Code:QVPSRPNRAP
Three Letter Code:H-Gln-Val-Pro-Ser-Arg-Pro-Asn-Arg-Ala-Pro-OH
Labeling Target
GTPase dynamin
Purity
>98 %
Activity
Inhibitor

Dynamin inhibitory peptide is a synthetic peptide compound designed to specifically interfere with the function of dynamin, a large GTPase critically involved in membrane fission events such as endocytosis. As a tool for dissecting the molecular mechanisms of vesicular trafficking, this peptide targets the protein-protein interactions or GTPase activity essential for dynamin-mediated membrane scission. Its ability to selectively modulate dynamin function makes it a valuable resource for researchers studying cellular trafficking, signal transduction, and the regulation of membrane dynamics. The peptide's sequence and structure are typically modeled to mimic or disrupt key interaction motifs, allowing for precise experimental manipulation of dynamin-dependent processes in a variety of biological systems.

Endocytosis Research: The primary application of the dynamin inhibitory peptide lies in the investigation of clathrin-mediated endocytosis and related vesicular transport pathways. By effectively blocking dynamin's role in membrane constriction and fission, the peptide enables researchers to temporally and spatially dissect the stages of vesicle formation and internalization. This approach is instrumental in clarifying the requirement for dynamin activity in the uptake of receptors, nutrients, and signaling molecules, providing insights into how cells regulate surface composition and respond to extracellular cues.

Membrane Trafficking Studies: In the context of intracellular trafficking, inhibition of dynamin function allows for the analysis of post-endocytic sorting, recycling, and degradation routes. The peptide is frequently employed to differentiate between dynamin-dependent and -independent pathways, offering a means to map the fate of internalized cargo and the underlying molecular machinery. Such studies are essential for understanding the orchestration of vesicle budding, transport, and fusion within the endomembrane system, with implications for organelle biogenesis and maintenance.

Signal Transduction Analysis: Dynamin is known to participate in signaling cascades by regulating the internalization of key receptors and associated proteins. The inhibitory peptide serves as a strategic tool to uncouple endocytic events from downstream signaling, thereby enabling the dissection of signal propagation mechanisms. Researchers utilize this approach to evaluate how membrane trafficking influences the intensity, duration, and specificity of cellular responses to external stimuli, particularly in receptor tyrosine kinase and G-protein coupled receptor pathways.

Neuroscience and Synaptic Function: In neuronal systems, dynamin plays a pivotal role in synaptic vesicle recycling, which is fundamental for neurotransmitter release and synaptic plasticity. The peptide is employed in experimental models to inhibit synaptic endocytosis, allowing for detailed exploration of presynaptic mechanisms, neurotransmission dynamics, and the molecular basis of learning and memory. Its use facilitates the identification of compensatory pathways and the characterization of synaptic defects associated with impaired vesicle turnover.

High-Content Screening and Drug Discovery: The dynamin inhibitory peptide is also utilized in high-throughput screening platforms aimed at identifying small molecules or genetic modifiers that influence dynamin function or membrane trafficking. By serving as a reference inhibitor or positive control, the peptide helps validate assay sensitivity and specificity, streamlining the discovery of novel regulators of endocytosis and vesicle dynamics. This application is particularly relevant for pharmaceutical research targeting diseases linked to dysregulated membrane trafficking, such as neurodegeneration and cancer.

Long-term Storage Conditions
Soluble in DMSO
Solubility
-20 °C
InChI
InChI=1S/C47H80N18O14/c1-23(2)35(62-36(69)25(48)14-15-33(49)67)44(77)64-19-7-12-31(64)41(74)61-29(22-66)39(72)59-27(10-5-17-56-47(53)54)43(76)63-18-6-11-30(63)40(73)60-28(21-34(50)68)38(71)58-26(9-4-16-55-46(51)52)37(70)57-24(3)42(75)65-20-8-13-32(65)45(78)79/h23-32,35,66H,4-22,48H2,1-3H3,(H2,49,67)(H2,50,68)(H,57,70)(H,58,71)(H,59,72)(H,60,73)(H,61,74)(H,62,69)(H,78,79)(H4,51,52,55)(H4,53,54,56)/t24-,25-,26-,27-,28-,29-,30-,31-,32-,35-/m0/s1
InChI Key
LHQOQXYEPUSHJL-LNIRUYPRSA-N
Isomeric SMILES
C[C@@H](C(=O)N1CCC[C@H]1C(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(=O)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@@H]3CCCN3C(=O)[C@H](C(C)C)NC(=O)[C@H](CCC(=O)N)N
BoilingPoint
N/A
Melting Point
N/A

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