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 Chemical Structure

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)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (53.13 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.5313 mL 2.6563 mL 5.3127 mL
5 mM 0.1063 mL 0.5313 mL 1.0625 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.1%

SDS (393 KB)

COA (245 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.5313 mL 2.6563 mL 5.3127 mL 13.2817 mL
5 mM 0.1063 mL 0.5313 mL 1.0625 mL 2.6563 mL
10 mM 0.0531 mL 0.2656 mL 0.5313 mL 1.3282 mL
15 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8854 mL
20 mM 0.0266 mL 0.1328 mL 0.2656 mL 0.6641 mL
25 mM 0.0213 mL 0.1063 mL 0.2125 mL 0.5313 mL
30 mM 0.0177 mL 0.0885 mL 0.1771 mL 0.4427 mL
40 mM 0.0133 mL 0.0664 mL 0.1328 mL 0.3320 mL
50 mM 0.0106 mL 0.0531 mL 0.1063 mL 0.2656 mL
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Gramicidin A Related Classifications

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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