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Art. -Nr.: HY-N19739

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Efrapeptin F

Efrapeptin F is a mitochondrial complex V inhibitor and cytotoxic agent with in vivo antitumor activity. Efrapeptin F induces cell death in glucose-limiting conditions, with preferential cytotoxicity to nutrient-deprived cancer cells under hypoxic conditions. Efrapeptin F can be used for the research of pancreatic cancer, prostate cancer, breast cancer, central nervous system cancer, colon cancer, lung cancer, melanoma, ovarian cancer, kidney cancer, stomach cancer.

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CAS. Nr.: 131353-66-7
Formel: C₈₂H₁₄₁N₁₈O₁₆⁺
Molecular Weight:1635.11

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Efrapeptin F Chemical Structure

CAS. Nr.: 131353-66-7

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	EC₅₀	25 μM Compound: 53	Cytotoxicity against human HepG2 cells assessed as decrease in cell viability measured after 48 hrs by MTS assay Cytotoxicity against human HepG2 cells assessed as decrease in cell viability measured after 48 hrs by MTS assay	[PMID: 33565879]
PANC-1	IC₅₀	52 nM Compound: Efrapeptin F	Anticancer activity against human PANC-1 cells assessed as reduction in cell viability by measuring ATP level incubated for 24 hrs by CellTiter-Glo assay Anticancer activity against human PANC-1 cells assessed as reduction in cell viability by measuring ATP level incubated for 24 hrs by CellTiter-Glo assay	[PMID: 32942072]

In Vitro

Efrapeptin F (0.001-10 μmol/L; 24 h) potently inhibits the survival of glucose-deprived human pancreatic cancer PANC-1 cells with an IC₅₀ of 0.052 μmol/L, which is over 100 times more potent than its effect on PANC-1 cells in nutrient-sufficient medium^[1].
Efrapeptin F (0.001-10 μmol/L; 24 h) exhibits preferential cytotoxicity to human pancreatic cancer PANC-1 cells under glucose-limiting conditions (≤100 mg/L glucose), regardless of amino acid or serum availability^[1].
Efrapeptin F (0.001-10 μmol/L; 24 h under 1% O₂) exhibits preferential cytotoxicity to glucose-deprived human pancreatic cancer PANC-1 cells under hypoxic (1% O₂) conditions, similar to its effect under normoxic conditions^[1].
Efrapeptin F (0.06 μmol/L; 24 h) causes a 100-fold reduction in cellular ATP levels in glucose-deprived human pancreatic cancer PANC-1 cells, but only a minor reduction in nutrient-sufficient PANC-1 cells^[1].
Efrapeptin F potently inhibits the growth of diverse human cancer cell lines in the JFCR39 panel, with a mean GI₅₀ of 135 nmol/L, and shows high potency (GI₅₀ = 1 nmol/L) against multiple breast, central nervous system, lung, ovarian, stomach, and prostate cancer cell lines^[1].
Efrapeptin F (0.1 μmol/L; 24 h) induces significant early and late apoptosis in glucose-deprived human pancreatic cancer PANC-1 cells, but not in nutrient-sufficient PANC-1 cells^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

human pancreatic cancer PANC-1 cells
Concentration:

0.001, 0.01, 0.1, 1, 10 μmol/L
Incubation Time:

24 h
Result:

Exhibited preferential cytotoxicity to PANC-1 cells in nutrient-deprived medium (NDM (-)) with an IC₅₀ of 0.052 μmol/L.
Showed an IC₅₀ of >10 μmol/L in nutrient-sufficient DMEM (10% FBS), making the cytotoxic effect over 100 times stronger under glucose-deprived conditions.

Apoptosis Analysis^[1]

Cell Line:

human pancreatic cancer PANC-1 cells
Concentration:

0.1 μmol/L
Incubation Time:

24 h
Result:

Resulted in 99% viable cells, 0% early apoptotic cells, 1% late apoptotic cells, and 0% necrotic cells in nutrient-sufficient DMEM (10% FBS).
Induced 22% viable cells, 43% early apoptotic cells, 31% late apoptotic cells, and 4% necrotic cells in glucose-deprived NDM (-), representing a significant increase in apoptotic cell death.

Cell Viability Assay^[1]

Cell Line:

human pancreatic cancer PANC-1 cells
Concentration:

0.001, 0.01, 0.1, 1, 10 μmol/L
Incubation Time:

24 h
Result:

Induced preferential cell death in PANC-1 cells only under glucose-deprived conditions, regardless of the presence or absence of amino acids and serum.
Showed no cytotoxicity in media with 1000 or 500 mg/L glucose, but exhibited cytotoxicity in media with glucose concentrations ≤100 mg/L.

Cell Cytotoxicity Assay^[1]

Cell Line:

human pancreatic cancer PANC-1 cells
Concentration:

0.001, 0.01, 0.1, 1, 10 μmol/L
Incubation Time:

24 h (under 1% O₂ hypoxic conditions)
Result:

Showed preferential cytotoxicity to PANC-1 cells in glucose-deprived NDM (-) under hypoxic conditions, with a sharp reduction in cell survival at concentrations ≥0.1 μmol/L.
Maintained high cell survival in nutrient-sufficient DMEM (10% FBS) under the same hypoxic conditions.

In Vivo

Efrapeptin F (0.0625-0.125 mg/kg; i.v.; twice weekly; 3 weeks) reduces PC-3 prostate cancer xenograft tumor weight by 31% and 14%, respectively, without significant body weight loss in most treated mice^[1].

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

Animal Model:

SCID (male, 6 weeks old, human prostate cancer PC-3 cells subcutaneously injected)^[1]
Dosage:

0.125 mg/kg; 0.0625 mg/kg
Administration:

i.v.; twice weekly; 3 weeks
Result:

Reduced mean tumor weight by 31% relative to control (0.63 g vs control 0.92 g) at 0.125 mg/kg.
Reduced mean tumor weight by 14% relative to control (0.79 g vs control 0.92 g) at 0.0625 mg/kg.
Did not reduce body weight of treated mice at tested doses.
Resulted in one death at day 23 in the 0.125 mg/kg group, with remaining 6 mice surviving until study end without anatomical toxic effects in critical organs.

Chemical Information

CAS. Nr. 131353-66-7
Molecular Weight 1635.11
Formel C₈₂H₁₄₁N₁₈O₁₆⁺
SMILES

O=C([C@H]1N(CCCC1)C(C(C)(C)NC(C(C)(C)NC(CNC(CCNC([C@H](CC(C)C)NC(C(C)(C)NC(C(C)(C)NC([C@H]2N(CCCC2)C(C(C)(C)NC([C@H]3N(CCCC3)C(C)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)NC(C)(C)C(N[C@@H](C)C(N[C@@H](CC(C)C)C(N[C@](CC)(C)C(N[C@@H](CC(C)C)C[N+]4=C5N(CCC4)CCC5)=O)=O)=O)=O
Structure Classification
- Peptides
Initial Source
- Microorganisms
Tolypocladium fungi
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Momose I, et al. Mitochondrial inhibitors show preferential cytotoxicity to human pancreatic cancer PANC-1 cells under glucose-deprived conditions. Biochemical and biophysical research communications. 2010 Feb 12;392(3):460-6. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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MOQ

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