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MedChemExpress - Model Gramicidin A - 11029-61-1

Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α)[1][2].

Gramicidin A

MCE China：Gramicidin A

Brand：MedChemExpress (MCE)

Cat. No.HY-P2324

CAS：11029-61-1

Purity：98.10%

Storage：Sealed storage, away from moisture Powder -80°C 2 years -20°C 1 year *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).

In Vitro：Gramicidin A displays potent broad-spectrum antibiotic activity against Gram-positive strains, even multidrug-resistant strains[1]. Gramicidin A has the disadvantage of high hemolytic activity[1]. Gramicidin A (0.1 nM-10 μM, 72 h) reduces the viability of RCC cell lines and affects cell viability comparable to Monensin (HY-N4302)[2]. Gramicidin A cellular sensitivity is significantly altered by neither VHL nor HIF-1α expression[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, reduces HIF transcriptional activity and target gene expression (24 h)[3]

In Vivo：Gramicidin A (0.11 mg/kg; intratumoral injection; twice weekly for 14 days) inhibits the growth of RCC tumor xenografts[2]. Gramicidin A (0.22 mg/kg; intratumoral injection; thrice weekly for 26 days) inhibits the growth and angiogenesis of VHL-expressing RCC tumor xenografts[3].

IC50 & Target：HIF-1α[2] In Vitro Gramicidin A displays potent broad-spectrum antibiotic activity against Gram-positive strains, even multidrug-resistant strains[1]. Gramicidin A has the disadvantage of high hemolytic activity[1]. Gramicidin A (0.1 nM-10 μM, 72 h) reduces the viability of RCC cell lines and affects cell viability comparable to Monensin (HY-N4302)[2]. Gramicidin A cellular sensitivity is significantly altered by neither VHL nor HIF-1α expression[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, reduces HIF transcriptional activity and target gene expression (24 h)[3] MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Gramicidin A Related Antibodies Cell Viability Assay[2] Cell Line: A498, 786-O, Caki-1, SN12C, ACHN, UMRC6, UMRC6+VHL, HEK293T+pcDNA3, HEK293T+HA-HIF-1α, HEK293T+HA-HIF-1α-mut

Sequence：{For}-Val-Gly-Ala-{D-Leu}-Ala-{D-Val}-Val-{D-Val}-Trp-{D-Leu}-Trp-{D-Leu}-Trp-{D-Leu}-Trp-{NHCH2CH2OH}

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 Oct 1;11(1):4935. [Content Brief]

[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 Nov;12(11):2296-307. [Content Brief]

[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 Apr;13(4):788-99. [Content Brief]

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