MCE Bryostatin 1 ≥99.0%, from bryozoan Bugula neritina , 10 μg

Bryostatin 1 is a naturally occurring marine macrolide isolated from the bryozoan Bugula neritina. It is a potent, central nervous system (CNS)–permeable protein kinase C (PKC) modulator, widely studied for its neuroprotective, anti-cancer, anti-inflammatory, and anti-HIV properties.

Bryostatin 1 directly interacts with the C1 domain of Munc13-1, a key presynaptic regulatory protein, with dissociation constants (Ki) of 8.07 nM for the isolated C1 domain and 0.45 nM for the full-length protein. This high-affinity binding underlies its role in regulating synaptic transmission, neuronal signaling, and immune responses.

Mechanism of Action

Bryostatin 1 functions primarily as a PKC modulator, influencing intracellular signaling pathways through PKC activation and downstream cellular processes.

It also modulates synaptic signaling through Munc13-1 translocation, affecting neurotransmitter release and synaptic plasticity. Due to its CNS permeability, it is actively investigated in neurodegenerative disease models and cognitive research.

In addition, Bryostatin 1 has demonstrated anti-HIV-1 effects and plays a role in immune system modulation, particularly through TLR4 signaling pathways in dendritic cells.

Biological Activity

In Vitro Activity

• In HT22 neuronal cells (1 μM, 5 minutes), Bryostatin 1 induces rapid recruitment of Munc13-1 from the cytosol to the plasma membrane.
• Similar translocation effects are observed with ubMunc13-2 and bMunc13-2 proteins.
• After 24 hours incubation, Bryostatin 1 increases the expression levels of Munc13-1 in both HT22 cells and primary mouse hippocampal neurons.
• It also modulates immune responses by influencing dendritic cell signaling via the TLR4 MyD88-independent pathway, promoting anti-inflammatory, Th2-skewed immune differentiation.

In Vivo Activity

In C57BL/6J mouse models, Bryostatin 1 administered at 30 µg/kg intraperitoneally, 3 days per week for 2 weeks effectively prevented the onset of experimental autoimmune encephalomyelitis (EAE), demonstrating potential therapeutic relevance in neuroinflammatory conditions.

Applications

Bryostatin 1 is widely used in research involving:

• Neurodegenerative diseases (Alzheimer’s disease, cognitive decline)
• Synaptic plasticity and memory research
• Protein kinase C pathway studies
• HIV latency and viral reactivation studies
• Cancer research and signal transduction
• Immunology and T-cell modulation
• Neuroinflammation models
• CNS drug development research

Key Properties

Bryostatin 1 is a highly potent and CNS-active natural modulator of PKC and Munc13-1, offering significant value in neuroscience, immunology, and oncology research. Its multifaceted biological properties make it an essential compound in studies investigating synaptic function, neuroinflammation, cancer signaling, and viral latency.