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Submit ReviewPlitidepsin (dehydrodidemnin B) is a potent inhibitor of protein synthesis, blocker of G1 and G2 phases in cell cycle and potent antiviral against SARS-CoV-2 in hACE2-293T, Vero E6 cells and models of pneumocyte-like cells (IC90 values are 0.88 nM, 1.76 nM and 3.14 nM, respectively). Plitidepsin also inhibits eukaryotic translation elongation factor 1 alpha 1 (eEF1A) (KD = 80 nM).
In vitro, it inhibits induction of ornithine decarboxylase (ODC), which is essential for cell transformation and proliferation.
In vivo, daily administration of Plitidepsin on mice affected by Ehrlich carcinoma duplicated the animal life-span and decreased the total number of tumor cells by 70-90%. Plitidepsin also reduces viral SARS-CoV-2 replication in the lungs (mouse).
It is recommended to prepare stock solutions in DMSO.
| M. Wt | 1110.36 |
| Formula | C57H87N7O15 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 137219-37-5 |
| PubChem ID | 9812534 |
| InChI Key | UUSZLLQJYRSZIS-LXNNNBEUSA-N |
| Smiles | [H][C@@]12CCCN1C([C@](CC(C)C)(NC([C@H](C([C@H](C(C)C)OC(C[C@@H]([C@](NC([C@H]([C@H](OC([C@@H](N(C2=O)C)CC3=CC=C(C=C3)OC)=O)C)NC([C@H](N(C([C@@H]4CCCN4C(C(C)=O)=O)=O)C)CC(C)C)=O)=O)([C@H](CC)C)[H])O)=O)=O)C)=O)[H])=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Urdiales et al (1996) Antiproliferative effect of dehydrodidemnin B (DDB), a depsipeptide isolated from Mediterranean tunicates. Cancer Letters 102 31 PMID: 8603376
Losada et al (2016) Translation elongation factor eEF1A2 is a novel anticancer target for the marine natural product plitidepsin. Sci.Rep. 6 PMID: 27713531
White et al (2021) Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A. Science 371 926 PMID: 33495306
Reuschl et al (2021) Host-directed therapies against early-lineage SARS-CoV-2 retain efficacy against B.1.1.7 variant. bioRxiv PMID: 33501437
If you know of a relevant reference for Plitidepsin, please let us know.
Keywords: Plitidepsin, Plitidepsin supplier, Plitidepsin, DDB, Dehydrodidemnin, B, Aplidin, potent, selective, inhibitor, inhibits, protein, synthesis, eEF1A, antiviral, SARS, COV, 2, Covid, virus, reduces, viral, replication, antitumor, anticancer, proliferation, ornithine, decarboxylase, lung, cells, Ehrlich, carcin, DNA,, RNA, and, Protein, Synthesis, COVID-19, Coronavirus, Cell, Cycle, Inhibitors, 7416, Tocris Bioscience
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