Gramicidin A
Based on 1 publication(s) in Google Scholar
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).
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- Reinheit : 92.5%
- CAS. Nr.: 11029-61-1
- Formel: C99H140N20O17
- Molecular Weight:1882.29
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Speicherung:
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)
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Biologische Aktivität
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Chemical Information
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MK-8617HIF PHD1-3 Inhibitor -
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SYP-5 (Standard)HIF-1 Inhibitor
Publications Citing Use of MedChemExpress (MCE) Gramicidin A
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Biologische Aktivität
Beschreibung
IC50 & Target
HIF-1α[2]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
98.83 μM
Compound: GNF-Pf-2578
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[PMID: 18579783] |
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. .
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Cell Line:A498, 786-O, Caki-1, SN12C, ACHN, UMRC6, UMRC6+VHL, HEK293T+pcDNA3, HEK293T+HA-HIF-1α, HEK293T+HA-HIF-1α-mut
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Concentration:0.1 nM-10 μM
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Incubation Time:72 h
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Result:Reduced the viability with IC50s of 0.420, 0.430, 0.228, 0.104, 0.783, 0.253, 0.425, 0.057, 0.058 and 0.067 μM against A498, 786-O, Caki-1, SN12C, ACHN, UMRC6, UMRC6+VHL, HEK293T+pcDNA3, HEK293T+HA-HIF-1α, HEK293T+HA-HIF-1α-mut cells, respectively.
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Cell Line:786-O, SN12C, Caki-1, ACHN
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Concentration:1 and 10 μM or 0.1, 0.5 and 1.0 μM
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Incubation Time:24, 48 or 72 h
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Result:PARP cleavage was not detected. Increased the phosphorylation of AMPKα and its substrate ACC at both 24 and 48 hours. Reduced HIF-1α and HIF-2α protein expression. Hypoxic expression of CA-IX, GLUT-1, and GAPDH were all decreased in a dose-dependent manner.
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Cell Line:SN12C, Caki-1, ACHN
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Concentration:0.1, 0.5 and 1.0 μM
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Incubation Time:24 h
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Result:Significantly altered transcript expression for only HIF-2α in SN12C cells.
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female hairless Nu/J mice, 6- to 8-week old, injected subcutaneously with a suspension of SN12C cells (1.0 × 106) in a 50% growth factor–reduced Matrigel solution[2]
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Dosage:0.11 mg/kg body weight
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Administration:Intratumoral injection, twice weekly for 14 days
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Result:The average tumor mass was reduced by approximately 40% without significant toxicity.
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Animal Model:Female hairless 6- to 8-week-old Nu/J mice, injected subcutaneously with a suspension of Caki-1-td-Tomato cells (1.5 × 106) in a 50% growth factor-reduced Matrigel solution[3].
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Dosage:0.22 mg/kg
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Administration:Intratumoral injection, thrice weekly for 26 days
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Result:Inhibited tumor growth. HIF-2α and GAPDH protein expression was substantially reduced.
Chemical Information
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CAS. Nr. 11029-61-1
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Appearance Solid
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Molecular Weight 1882.29
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Formel C99H140N20O17
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Color White to off-white
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Sequence
{For}-Val-Gly-Ala-{D-Leu}-Ala-{D-Val}-Val-{D-Val}-Trp-{D-Leu}-Trp-{D-Leu}-Trp-{D-Leu}-Trp-{NHCH2CH2OH}
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
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)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
Direct activation of KCC2 arrests benzodiazepine refractory status epilepticus and limits the subsequent neuronal injury in mice. [Abstract]2023 Mar 21;4(3):100957. PMID: 36889319
Reinheit & Dokumentation
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Data Sheet (269 KB)
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SDS (393 KB)
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- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Gramicidin A Related Classifications
HY-P2324 Related Classifications
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