1. Apoptosis Anti-infection
  2. Ferroptosis Antibiotic
  3. Emodinanthrone

Emodinanthrone (EmodAn) is a MARCH7 stabilizer that inhibits ferroptosis (EC50=70 nM). Emodinanthrone is also a precursor to Emodin (HY-14393) and possesses antibiotic activity. Emodinanthrone directly binds to MARCH7 and blocks its ubiquitination-mediated degradation at the K608 site; this action enhances MARCH7-mediated K48 ubiquitination and degradation of NCOA4, as well as its regulation of the intracellular localization of TFR1 via K63 ubiquitination, thereby reducing the intracellular labile iron pool and blocking ferroptosis. Emodinanthrone demonstrates in vivo cardioprotective effects and exhibits a favorable safety profile. Emodinanthrone is applicable to research on ferroptosis-related cardiovascular diseases, including Doxorubicin (HY-15142A)-induced cardiomyopathy and myocardial ischemia-reperfusion injury.

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Emodinanthrone

Emodinanthrone Chemical Structure

CAS No. : 491-60-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

Emodinanthrone (EmodAn) is a MARCH7 stabilizer that inhibits ferroptosis (EC50=70 nM). Emodinanthrone is also a precursor to Emodin (HY-14393) and possesses antibiotic activity. Emodinanthrone directly binds to MARCH7 and blocks its ubiquitination-mediated degradation at the K608 site; this action enhances MARCH7-mediated K48 ubiquitination and degradation of NCOA4, as well as its regulation of the intracellular localization of TFR1 via K63 ubiquitination, thereby reducing the intracellular labile iron pool and blocking ferroptosis. Emodinanthrone demonstrates in vivo cardioprotective effects and exhibits a favorable safety profile. Emodinanthrone is applicable to research on ferroptosis-related cardiovascular diseases, including Doxorubicin (HY-15142A)-induced cardiomyopathy and myocardial ischemia-reperfusion injury[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
HaCaT IC50
> 5 μM
Compound: 5k
Antiproliferative (inhibition of cell growth) activity against HaCaT cells (human keratinocyte line)
Antiproliferative (inhibition of cell growth) activity against HaCaT cells (human keratinocyte line)
[PMID: 9371243]
KB IC50
3.9 μM
Compound: emodin anthrone
Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
[PMID: 11575949]
In Vitro

Emodinanthrone (5 μM; 12 h) inhibits RSL3 (0.20 μM)-induced ferroptosis in HT-1080 cells, enhances cell viability, and reduces intracellular Fe2+ and lipid ROS levels[1].
Emodinanthrone (0.3125-5 μM; 12 h) dose-dependently enhances the viability of RSL3 (0.20 μM)-treated HT-1080 cells, exhibiting an anti-ferroptotic EC50 of 70 nM; it also demonstrates cytotoxicity against HT-1080 and HeLa cells, with IC50 values ??of 35.58 μM and 19.40 μM, respectively[1].
Emodinanthrone (5 μM; 12 h) fails to inhibit RSL3-induced ferroptosis in MARCHF7-knockdown/knockout HT-1080 cells, nor does it reduce lipid ROS levels in these cells[1].
Emodinanthrone (5 μM; 24 h) inhibits the RSL3-induced ubiquitination-mediated degradation of MARCH7 in HT-1080 cells, thereby stabilizing the MARCH7 protein, while having no effect on the ubiquitination and degradation of the MARCH7-K608R mutant[1].
Emodinanthrone (5 μM; 24 h) stabilizes the MARCH7 protein in HeLa cells and downregulates NCOA4 while upregulating the protein levels of FTH1 and GPX4[1].
Emodinanthrone (5 μM; 24 h) enhances the GFP-MARCH7 fluorescence signal in HeLa-GFP-MARCH7 cells, thereby stabilizing the MARCH7 protein[1].

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

Cell Viability Assay[1]

Cell Line: HT-1080
Concentration: 0.3125 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM
Incubation Time: 24 h
Result: Showed no obvious cytotoxicity in normal HT-1080 cells, with an IC50 of 35.58 μM.
Dose-dependently increased cell viability in RSL3 (0.20 μM)-treated HT-1080 cells, with an anti-ferroptosis EC50 of 70 nM.
Significantly reversed RSL3-induced ferroptosis and cell viability reduction.
In Vivo

Emodinanthrone (0.5, 1, 2 mg/kg; i.p.; once daily; for 7 consecutive days) in Normal C57BL/6J male mice, did not affect mouse body weight, organ weights, liver and kidney function, or cardiac biochemical parameters; no significant toxic side effects observed[1].
Emodinanthrone (1 mg/kg; i.p.; 72 h prior to DOX modeling and continued for 3 days; and an additional 14 days) in Doxorubicin (DOX)-induced cardiomyopathy model in C57BL/6J male mice, induces serum levels of CK-MB, AST, and LDH; alleviates myocardial inflammation and fibrosis; reduces myocardial iron overload and lipid ROS; restores myocardial expression of MARCH7, GPX4, and FTH1 while downregulating NCOA4; and improves mouse survival rate[1].
Emodinanthrone (1 mg/kg; i.p.; once as a pretreatment prior to I/R modeling) in Myocardial Ischemia-Reperfusion (I/R) injury model in C57BL/6J male mice, reduces serum levels of AST, CK-MB, BUN, CK, and LDH; alleviates myocardial inflammation and fibrosis; reduces myocardial iron overload and lipid ROS; and restores myocardial expression of MARCH7, GPX4, and FTH1 while downregulating NCOA4[1].

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

Molecular Weight

256.25

Formula

C15H12O4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(C=C(C)C=C2O)CC3=CC(O)=CC(O)=C13

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (65.05 mM; ultrasonic and warming and heat to 80°C; 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 3.9024 mL 19.5122 mL 39.0244 mL
5 mM 0.7805 mL 3.9024 mL 7.8049 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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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: 98.66%

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 (protect from light). 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 3.9024 mL 19.5122 mL 39.0244 mL 97.5610 mL
5 mM 0.7805 mL 3.9024 mL 7.8049 mL 19.5122 mL
10 mM 0.3902 mL 1.9512 mL 3.9024 mL 9.7561 mL
15 mM 0.2602 mL 1.3008 mL 2.6016 mL 6.5041 mL
20 mM 0.1951 mL 0.9756 mL 1.9512 mL 4.8780 mL
25 mM 0.1561 mL 0.7805 mL 1.5610 mL 3.9024 mL
30 mM 0.1301 mL 0.6504 mL 1.3008 mL 3.2520 mL
40 mM 0.0976 mL 0.4878 mL 0.9756 mL 2.4390 mL
50 mM 0.0780 mL 0.3902 mL 0.7805 mL 1.9512 mL
60 mM 0.0650 mL 0.3252 mL 0.6504 mL 1.6260 mL
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  • 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.

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Emodinanthrone
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HY-N9362
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