Plitidepsin

Plitidepsin is a depsipeptide that was originally isolated from Aplidium albicans and has diverse biological activities. It binds to the alpha subunit isoform eEF1A2 of eukaryotic elongation factor 1 (eEF1, Kd = 79 nM) and inhibits the proliferation of NCI H460 non-small cell lung cancer (NSCLC) and HGC-27 gastric cancer cells (IC50s = 0.2 and 0.9 nM, respectively). Plitidepsin (0.01 nM) inhibits bone resorption by osteoclasts in a pit formation assay using bovine bone slices. It reduces viral titers and lung inflammation in the K18-hACE2 mouse model of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection when administered at a dose of 0.3 mg/kg.Formal Name: N-[1-(1,2-dioxopropyl)-L-prolyl]-didemnin A. CAS Number: 137219-37-5. Synonyms: Aplidin, Dehydrodidemnin B. Molecular Formula: C57H87N7O15. Formula Weight: 1110.3. Purity: >98%. Formulation: (Request formulation change), A solution in acetonitrile. Solubility: DMSO: soluble. SMILES: O=C1N2[C@](CCC2)([H])C(N([C@H](C(O[C@@H]([C@@H](C(N[C@]([C@H](CC(O[C@H](C([C@@H](C(N[C@H]1CC(C)C)=O)C)=O)C(C)C)=O)O)([H])[C@@H](C)CC)=O)NC([C@@H](CC(C)C)N(C)C([C@H]3N(C(C(C)=O)=O)CCC3)=O)=O)C)=O)CC4=CC=C(C=C4)OC)C)=O. InChi Code: InChI=1S/C57H87N7O15/c1-15-33(8)46-44(66)29-45(67)79-49(32(6)7)48(68)34(9)50(69)58-39(26-30(2)3)54(73)64-25-17-19-41(64)56(75)62(13)43(28-37-20-22-38(77-14)23-21-37)57(76)78-36(11)47(52(71)59-46)60-51(70)42(27-31(4)5)61(12)55(74)40-18-16-24-63(40)53(72)35(10)65/h20-23,30-34,36,39-44,46-47,49,66H,15-19,24-29H2,1-14H3,(H,58,69)(H,59,71)(H,60,70)/t33-,34-,36+,39-,40-,41-,42+,43-,44-,46+,47-,49-/m0/s1. InChi Key: UUSZLLQJYRSZIS-LXNNNBEUSA-N. Origin: Synthetic.