2. Anti-infection Metabolic Enzyme/Protease
  3. Bacterial HIF/HIF Prolyl-Hydroxylase Antibiotic
  4. Gramicidin A

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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Gramicidin A

Gramicidin A Chemical Structure

CAS No. : 11029-61-1

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Based on 1 publication(s) in Google Scholar

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Gramicidin A Related Antibodies

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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)[1][2].

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.

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
Concentration: 0.1 nM-10 μM
Incubation Time: 72 h
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.

Western Blot Analysis[2][3]

Cell Line: 786-O, SN12C, Caki-1, ACHN
Concentration: 1 and 10 μM or 0.1, 0.5 and 1.0 μM
Incubation Time: 24, 48 or 72 h
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.

RT-PCR[3]

Cell Line: SN12C, Caki-1, ACHN
Concentration: 0.1, 0.5 and 1.0 μM
Incubation Time: 24 h
Result: Significantly altered transcript expression for only HIF-2α in SN12C cells.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 0.11 mg/kg body weight
Administration: Intratumoral injection, twice weekly for 14 days
Result: The average tumor mass was reduced by approximately 40% without significant toxicity.
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].
Dosage: 0.22 mg/kg
Administration: Intratumoral injection, thrice weekly for 26 days
Result: Inhibited tumor growth. HIF-2α and GAPDH protein expression was substantially reduced.
Molecular Weight

1882.29

Formula

C99H140N20O17
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

{For}-Val-Gly-Ala-{D-Leu}-Ala-{D-Val}-Val-{D-Val}-Trp-{D-Leu}-Trp-{D-Leu}-Trp-{D-Leu}-Trp-{NHCH2CH2OH}
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Purity & Documentation

Purity: 98.1%

SDS (393 KB)

COA (245 KB)

Handling Instructions (2659 KB)
References
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Gramicidin A Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gramicidin A11029-61-1BacterialHIF/HIF Prolyl-HydroxylaseAntibioticHypoxia-inducible factorsHIFsHIF-PHrenal cell carcinomaRCC786-OSN12CantitumorangiogenesisInhibitorinhibitorinhibit

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