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Bryostatin 1 is a marine macrolide that has been found in B. neritina and has diverse biological activities.1,2,3,4,5 It binds to PKCα, PKCβ1, PKCγ, PKCδ, PKCε, PKCη, and PKCθ (Kis = 0.8-3.0 nM) and induces PKC activation or inhibition in cancer cells in a concentration-dependent manner.1,2 Bryostatin 1 (50 nM) reduces the production of IL-2 and increases the production of IL-10 in LPS-stimulated mouse bone marrow-derived dendritic cells (BMDCs).1 It decreases cell surface levels of CD4 and chemokine (C-C motif) receptor 5 (CCR5) and reduces HIV-1 infectivity in isolated human monocyte-derived macrophages.3 In vivo, bryostatin 1 (30 µg/kg) reduces spinal cord and brain T cell infiltration and disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).4 It also decreases blast-induced increases in blood-brain barrier (BBB) permeability in a rat model of traumatic brain injury (TBI) when administered at a dose of 2.5 mg/kg.5
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1. Designed PKC-
2. Bryostatin-
3. Bryostatin-
4. Bryostatin-
5. Bryostatin-