Bryostatin 1

• CAT Number: M020085
• CAS Number: 83314-01-6
• Molecular Formula: C47H68O17
• Molecular Weight: 905.04
• Purity: ≥95%
• Target: PKC
• Solubility: Soluble in DMSO > 10 mM
• Storage: Store at -20°C
• InChIKey: MJQUEDHRCUIRLF-UHFFFAOYSA-N
• SMILES: CCCC=CC=CC(=O)OC1C(=CC(=O)OC)CC2CC(OC(=O)CC(CC3CC(C(C(O3)(CC4CC(=CC(=O)OC)CC(O4)C=CC(C1(O2)O)(C)C)O)(C)C)OC(=O)C)O)C(C)O

Bryostatin 1 is a potent modulator of protein kinase C (PKC).

It showed activity in laboratory tests in cells and model animals, so it was brought into clinical trials. As of 2014 over thirty clinical trials had been conducting, using bryostatin alone and in combination with other agents, in both solid tumors and blood tumors; it did not show a good enough risk:benefit ratio to be advanced further.

It showed enough promise in animal models of Alzheimer/’s disease that a Phase II trial was started by 2010; the trial was sponsored by the Blanchette Rockefeller Neurosciences Institute. Scientists from that institute started a company called Neurotrope, and launched another clinical trial in Alzheimer/’s disease, preliminary results of which were released in 2017.

Bryostatin has also been studied in people with HIV.

Reference

1: Making Bryostatin 1 through Smart Chemistry. Cancer Discov. 2017 Oct 24. doi:
10.1158/2159-8290.CD-NB2017-148. [Epub ahead of print] PubMed PMID: 29066536.

2: Wender PA, Hardman CT, Ho S, Jeffreys MS, Maclaren JK, Quiroz RV, Ryckbosch
SM, Shimizu AJ, Sloane JL, Stevens MC. Scalable synthesis of bryostatin 1 and
analogs, adjuvant leads against latent HIV. Science. 2017 Oct
13;358(6360):218-223. doi: 10.1126/science.aan7969. PubMed PMID: 29026042.

3: López-Huertas MR, Jiménez-Tormo L, Madrid-Elena N, Gutiérrez C, Rodríguez-Mora
S, Coiras M, Alcamí J, Moreno S. The CCR5-antagonist Maraviroc reverses HIV-1
latency in vitro alone or in combination with the PKC-agonist Bryostatin-1. Sci
Rep. 2017 May 24;7(1):2385. doi: 10.1038/s41598-017-02634-y. PubMed PMID:
28539614; PubMed Central PMCID: PMC5443841.

4: Alkon DL, Hongpaisan J, Sun MK. Effects of chronic bryostatin-1 on
treatment-resistant depression in rats. Eur J Pharmacol. 2017 Jul 15;807:71-74.
doi: 10.1016/j.ejphar.2017.05.001. Epub 2017 May 2. PubMed PMID: 28472666.

5: Dental C, Proust A, Ouellet M, Barat C, Tremblay MJ. HIV-1 Latency-Reversing
Agents Prostratin and Bryostatin-1 Induce Blood-Brain Barrier
Disruption/Inflammation and Modulate Leukocyte Adhesion/Transmigration. J
Immunol. 2017 Feb 1;198(3):1229-1241. doi: 10.4049/jimmunol.1600742. Epub 2016
Dec 19. PubMed PMID: 27994072.

6: Mizutani K, Sonoda S, Wakita H, Okazaki H, Katoh Y, Chihara T, Shimpo K.
Effects of exercise and bryostatin-1 on serotonin dynamics after cerebral
infarction. Neuroreport. 2016 Jun 15;27(9):659-64. doi:
10.1097/WNR.0000000000000592. PubMed PMID: 27128726.

7: Plummer S, Manning T, Baker T, McGreggor T, Patel M, Wylie G, Phillips D.
Isolation, analytical measurements, and cell line studies of the
iron-bryostatin-1 complex. Bioorg Med Chem Lett. 2016 May 15;26(10):2489-97. doi:
10.1016/j.bmcl.2016.03.099. Epub 2016 Mar 30. PubMed PMID: 27068183.