| Description | Gramicidin A is a peptide antibiotic isolated from B. brevis.Gramicidin A is a highly hydrophobic channel-forming ion carrier that forms monovalent cation-permeable channels in artificial membranes.Gramicidin A induces the degradation of hypoxia-inducible factor 1 alpha (HIF-1 alpha) and reduces the growth of a mouse xenograft model of human renal cell carcinoma. Gramicidin A has antibacterial, antimalarial and hemolytic activities. |
| In vitro | Gramicidin A (0.1 nM-10 μM; 72 h) reduces the viability of RCC cell lines and affects cell viability comparable to Monensin.[2] Gramicidin A (1 and 10 μM, 48 or 72 h) induces nonapoptotic cell death in RCC cells.[2] Gramicidin A (0-10 μM, 24 h) depletes cellular energy and induces metabolic dysfunction in RCC cells.[2] Gramicidin A (0-1 μM, 24-72 h) reduces HIF-1α and HIF-2α protein expression and reduces HIF transcriptional activity and target gene expression (24 h).[3] |
| In vivo | Gramicidin A (0.11 mg/kg; intratumoral injection; 2 weeks; 14 days) inhibits the growth of RCC tumor xenografts, the average tumor mass was reduced by approximately 40% without significant toxicity.[2] Gramicidin A (0.22 mg/kg; intratumoral injection; 3 weeks; 26 days) inhibits the growth and angiogenesis of VHL-expressing RCC tumor xenografts.[3] |
| Target activity | ACHN:0.783, Caki-1 cells:0.228 μM, 786-O:0.430 μM, SN12C:0.104 μM, A498:0.420 μM |
| molecular weight | 1882.29 |
| Molecular formula | C99H140N20O17 |
| CAS | 11029-61-1 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: Soluble H2O: Slightly soluble Ethanol: Soluble |
| References | 1. Takada Y, et al. Discovery of gramicidin A analogues with altered activities by multidimensional screening of a one-bead-one-compound library. Nat Commun. 2020;11(1):4935. 2. David JM, et al. Gramicidin A induces metabolic dysfunction and energy depletion leading to cell death in renal cell carcinoma cells. Mol Cancer Ther. 2013;12(11):2296-2307. 3. David JM, et al. Gramicidin A blocks tumor growth and angiogenesis through inhibition of hypoxia-inducible factor in renal cell carcinoma. Mol Cancer Ther. 2014;13(4):788-799. |