Cat. No.: HY-119694

Rotenolone

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Rotenolone is a metabolite of Rotenone (HY-B1756), inhibitor of Mitochondrial complex I, and antiproliferative agent, with an IC₅₀ of 137 nM against bovine complex I. Rotenolone undergoes biotransformation via multiple cytochrome P450 isoenzymes in rainbow trout liver microsomes. Rotenolone exhibits anticancer activity against ovarian cancer, breast cancer, prostate cancer, non-small cell lung cancer, and colon cancer. Rotenolone can be used in studies related to ovarian cancer, breast cancer, prostate cancer, non-small cell lung cancer, and colon cancer.

For research use only. We do not sell to patients.

Purity: 97.0%
CAS No.: 509-96-6
Formula: C₂₃H₂₂O₇
Molecular Weight:410.42

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Rotenolone Chemical Structure

CAS No.: 509-96-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

All Cytochrome P450 Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
697	IC₅₀	0.5 μM Compound: 7	Cytotoxicity against human 697 cells after 72 hrs by MTS assay Cytotoxicity against human 697 cells after 72 hrs by MTS assay	[PMID: 23895019]
697	IC₅₀	0.7 μM Compound: 7	Cytotoxicity against human 697 cells after 48 hrs by MTS assay Cytotoxicity against human 697 cells after 48 hrs by MTS assay	[PMID: 23895019]
A2780	IC₅₀	0.5 μg/mL Compound: 6	Cytotoxicity against human A2780 cells Cytotoxicity against human A2780 cells	[PMID: 15043430]
A2780	IC₅₀	0.95 μM Compound: 5	Antiproliferative activity against human A2780 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human A2780 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 20804165]
BT-549	IC₅₀	1.6 μM Compound: 5	Antiproliferative activity against human BT549 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human BT549 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 20804165]
DU-145	IC₅₀	2.7 μM Compound: 5	Antiproliferative activity against human DU145 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human DU145 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 20804165]
HCC 2998	IC₅₀	2.9 μM Compound: 5	Antiproliferative activity against human HCC2998 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human HCC2998 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 20804165]
HCT-116	IC₅₀	0.055 ug Compound: 6	Cytotoxicity against human HCT116 cells measured per disk after 5 days by hemocytometer counting Cytotoxicity against human HCT116 cells measured per disk after 5 days by hemocytometer counting	[PMID: 21452840]
HCT-116	IC₅₀	0.055 μg Compound: 6	Cytotoxicity against human HCT116 cells measured per disk after 5 days by hemocytometer counting Cytotoxicity against human HCT116 cells measured per disk after 5 days by hemocytometer counting	[PMID: 21452840]
HT-29	IC₅₀	0.1 μM Compound: 7	Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay	[PMID: 23895019]
NCI-H460	IC₅₀	2 μM Compound: 5	Antiproliferative activity against human NCI-H460 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human NCI-H460 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 20804165]
Raji	IC₅₀	2.4 μM Compound: 7	Cytotoxicity against human Raji cells after 72 hrs by MTS assay Cytotoxicity against human Raji cells after 72 hrs by MTS assay	[PMID: 23895019]
Raji	IC₅₀	5.6 μM Compound: 7	Cytotoxicity against human Raji cells after 48 hrs by MTS assay Cytotoxicity against human Raji cells after 48 hrs by MTS assay	[PMID: 23895019]
U-937	IC₅₀	0.07 μM Compound: 4, 12a-hydroxyrotenone	Antiproliferative activity against human U937 cells after 48 hrs by WST-8 assay Antiproliferative activity against human U937 cells after 48 hrs by WST-8 assay	[PMID: 17158054]
U-937	IC₅₀	0.09 μM Compound: 4, 12a-hydroxyrotenone	Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay	[PMID: 17158054]
U-937	IC₅₀	3.6 μM Compound: 4, 12a-hydroxyrotenone	Antiproliferative activity against human U937 cells after 24 hrs by WST-8 assay Antiproliferative activity against human U937 cells after 24 hrs by WST-8 assay	[PMID: 17158054]

In Vitro

Rotenolone potently inhibits proliferation of A2780 human ovarian cancer cells with an IC₅₀ of 0.95 μM^[2].
Rotenolone inhibits proliferation of BT-549 human breast cancer, DU 145 human prostate cancer, NCI-H460 human NSCLC, and HCC-2998 human colon cancer cells with IC₅₀ values of 1.6 μM, 2.7 μM, 2.0 μM, and 2.9 μM, respectively^[2].
Rotenolone inhibits bovine heart mitochondrial complex I with an IC₅₀ of 137 nM^[3].
Rotenolone is selectively cytotoxic to LNCaP prostate cancer cells with an ED₅₀ of 0.3-0.7 μM^[3].

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

Chemical Information

CAS No. 509-96-6
Appearance Solid
Molecular Weight 410.42
Formula C₂₃H₂₂O₇
Color White to off-white
SMILES

O=C1[C@@]2([C@]([H])(OC3=C1C=CC4=C3C[C@@H](O4)C(C)=C)COC5=C2C=C(C(OC)=C5)OC)O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (243.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4365 mL

12.1826 mL

24.3653 mL

5 mM

0.4873 mL

2.4365 mL

4.8731 mL

10 mM

0.2437 mL

1.2183 mL

2.4365 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Erickson D A, et al. Biotransformation of rotenone by hepatic microsomes following pretreatment of rainbow trout with inducers of cytochrome P450[J]. Pesticide biochemistry and physiology, 1992, 42(2): 140-150.

[2]. Harinantenaina L, et al. Antiproliferative compounds from Pongamiopsis pervilleana from the Madagascar Dry Forest. J Nat Prod. 2010;73(9):1559-1562. [Content Brief]

[3]. Russell DA, et al. Hydroxylated Rotenoids Selectively Inhibit the Proliferation of Prostate Cancer Cells. J Nat Prod. 2020;83(6):1829-1845. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.4365 mL	12.1826 mL	24.3653 mL	60.9132 mL
	5 mM	0.4873 mL	2.4365 mL	4.8731 mL	12.1826 mL
	10 mM	0.2437 mL	1.2183 mL	2.4365 mL	6.0913 mL
	15 mM	0.1624 mL	0.8122 mL	1.6244 mL	4.0609 mL
	20 mM	0.1218 mL	0.6091 mL	1.2183 mL	3.0457 mL
	25 mM	0.0975 mL	0.4873 mL	0.9746 mL	2.4365 mL
	30 mM	0.0812 mL	0.4061 mL	0.8122 mL	2.0304 mL
	40 mM	0.0609 mL	0.3046 mL	0.6091 mL	1.5228 mL
	50 mM	0.0487 mL	0.2437 mL	0.4873 mL	1.2183 mL
	60 mM	0.0406 mL	0.2030 mL	0.4061 mL	1.0152 mL
	80 mM	0.0305 mL	0.1523 mL	0.3046 mL	0.7614 mL
	100 mM	0.0244 mL	0.1218 mL	0.2437 mL	0.6091 mL

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Rotenolone

Metabolism/Protease Compound Library

Stem Cell Signaling Compound Library

Natural Product Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

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Oxygen Sensing Compound Library

Glutamine Metabolism Compound Library

Traditional Chinese Medicine Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

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Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

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Human Metabolite Library

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MCE Bioactive Compound Library

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Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

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High-Throughput Bioactive Compound Library

High-Throughput Natural Product Library

Mass Spectrometry Human Metabolite Library

Natural Product Diversity Scaffold Library

Mass Spectrometry Natural Product Library

All Cytochrome P450 Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Rotenolone Related Classifications

Cat. No.: HY-119694