Fig. 1 · Structure

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Rotenone

Cat. No. A10811 CAS 83-79-4

mitochondrial electron transport chain complex I inhibitor

Rotenone is an mitochondrial electron transport chain complex I inhibitor. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
697 IC50 0.3 μM Cytotoxicity against human 697 cells after 48 hrs by MTS assay [PMID: 23895019]
697 IC50 0.3 μM Cytotoxicity against human 697 cells after 72 hrs by MTS assay [PMID: 23895019]
A549 IC50 0.04 μg/mL Cytotoxicity against human A549 cells after 3 days by SRB assay [PMID: 16562843]
A549 IC50 0.901 μg/mL Cytotoxicity against human A549 cells by SRB assay [PMID: 22204911]
A549 ED50 26 μM Antitumor activity against human A549 cells after 24 hrs by MTT assay [PMID: 17482824]
BC1 cell line ED50 0.039 μg/mL Cytotoxicity against human BC1 cells after 72 hrs [PMID: 2614425]
Col2 ED50 0.15 μg/mL Cytotoxicity against human Col2 cells after 72 hrs [PMID: 2614425]
DU-145 IC50 0.465 μg/mL Cytotoxicity against human DU145 cells by SRB assay [PMID: 22204911]
HCT-116 IC50 0.045 ug Cytotoxicity against human HCT116 cells measured per disk after 5 days by hemocytometer counting [PMID: 21452840]
HeLa IC50 78 μM Cytotoxicity against human HeLa cells after 24 hrs by luminometry [PMID: 21741837]
HepG2 IC50 1.52 μM Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay [PMID: 30613327]
HepG2 ED50 15 μM Antitumor activity against human HepG2 cells after 24 hrs by MTT assay [PMID: 17482824]
HT-1080 ED50 0.047 μg/mL Cytotoxicity against human HT1080 cells after 48 hrs [PMID: 2614425]
HT-29 IC50 0.3 μM Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay [PMID: 23895019]
HT-29 ED50 202 μM Antitumor activity against human HT29 cells after 24 hrs by MTT assay [PMID: 17482824]
KB ED50 0.067 μg/mL Cytotoxicity against human KB cells after 72 hrs [PMID: 2614425]
KB IC50 0.513 μg/mL Cytotoxicity against human KB cells by SRB assay [PMID: 22204911]
L5178Y IC50 0.3 μM Cytotoxicity against mouse L5178Y cells by MTT assay [PMID: 28075580]
MCF7 IC50 0.008 μg/mL Cytotoxicity against human MCF7 cells after 3 days by SRB assay [PMID: 16562843]
MCF7 ED50 161 μM Antitumor activity against human MCF7 cells after 24 hrs by MTT assay [PMID: 17482824]
MES-SA ED50 147 μM Antitumor activity against human MES-SA cells after 24 hrs by MTT assay [PMID: 17482824]

21 records · Scroll to view more

In Vitro Studies

In cultured T cells, Rotenone alone at higher doses could transiently induce mitochondrial ROS. Rotenone treatment significantly reduced cancer cell invasion in the 4T1 and B16F10 models. In mitochondria isolated from Control-HCT 116 p53−/− cells, Rotenone treatment increased H2O2 release. [1,2,3]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Transient mitochondrial ROS induction in T cells

Cell-based study · T cells [1]

In cultured T cells, Rotenone alone at higher doses transiently induced mitochondrial ROS.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
MitoSOX staining of T cells, normalized to controlReported result rotenone alone at higher doses can transiently induce mitochondrial ROS[1]

Literature-Reported Treatment Conditions

Exposure duration
for either 5 hr or 6 days
Method
cultured in the indicated amounts of rotenone
Reported limits
Not stated in the sentences used: dose, vehicle.
Methods and source locations

Compound reported in the paper: Rotenone

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

RESULTS > ROS drives exhaustion by acting as a phosphatase inhibitor (S80); Extended Data Figure 6. legend (S269)

MitoSOX staining of T cells, normalized to control: MitoSOX staining of T cells, normalized to control; comparator: control — RESULTS > ROS drives exhaustion by acting as a phosphatase inhibitor (S80); Extended Data Figure 6. legend (S269)

Reduced cancer cell invasion

Cell-based study · 4T1 [2]

In 4T1 cells, Rotenone treatment significantly reduced invasion.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
invasionReported result significantly reduced invasion of cancer cells[2]

Literature-Reported Treatment Conditions

Method
rotenone treatment
Reported limits
Not stated in the sentences used: dose, schedule, vehicle, control.
Methods and source locations

Compound reported in the paper: Rotenone

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > PGC-1α expression determines invasive capacity and metastasis potential of cancer cells (S50, S53); Material and Methods > Invasion and migration assays (S164)

invasion: invasion — Results > PGC-1α expression determines invasive capacity and metastasis potential of cancer cells (S50, S53)

H2O2 release from isolated mitochondria

Cell-based study · mitochondria isolated from Control-HCT 116 p53−/− cells [3]

Rotenone treatment increased H2O2 release from mitochondria isolated from Control-HCT 116 p53−/− cells. H2O2 levels were measured using Amplex Red.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
H2O2 levels were measured using Amplex RedReported result 500 nM rotenone: increased the release of H2O2 from mitochondria isolated from Control-HCT 116 p53−/− cells[3]

Literature-Reported Treatment Conditions

Treatment concentration
500 nM
Method
Mitochondria were treated
Reported limits
Not stated in the sentences used: schedule, vehicle.
Methods and source locations

Compound reported in the paper: Rotenone

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results (S93, S96, S97, S98); Materials and methods > ROS measurements (S183, S184)

H2O2 levels were measured using Amplex Red: H2O2 levels were measured using Amplex Red; comparator: left untreated — Results (S93, S97, S98)

Reduced cancer cell invasion

Cell-based study · B16F10 [2]

In B16F10 cells, Rotenone treatment significantly reduced invasion.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
invasionReported result significantly reduced invasion of cancer cells[2]

Literature-Reported Treatment Conditions

Method
rotenone treatment
Reported limits
Not stated in the sentences used: dose, schedule, vehicle, control.
Methods and source locations

Compound reported in the paper: Rotenone

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > PGC-1α expression determines invasive capacity and metastasis potential of cancer cells (S50, S53); Material and Methods > Invasion and migration assays (S164)

invasion: invasion — Results > PGC-1α expression determines invasive capacity and metastasis potential of cancer cells (S50, S53)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 83-79-4
Applications mitochondrial electron transport chain complex I inhibitor
Formula C23H22O6
Molecular Weight 394.42
SMILES
O=C1[C@]2([H])[C@](COC3=CC(OC)=C(OC)C=C32)([H])OC4=C5C(O[C@@H](C(C)=C)C5)=CC=C14

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Scharping NE, Rivadeneira DB, Menk AV, et al. Mitochondrial stress induced by continuous stimulation under hypoxia rapidly drives T cell exhaustion. Nat Immunol (2021). PMID: 33398183 DOI: 10.1038/s41590-020-00834-9 Source material
  2. [2] LeBleu VS, O'Connell JT, Gonzalez Herrera KN, et al. PGC-1α mediates mitochondrial biogenesis and oxidative phosphorylation in cancer cells to promote metastasis. Nat Cell Biol (2014). PMID: 25241037 DOI: 10.1038/ncb3039 Source material
  3. [3] Wheaton WW, Weinberg SE, Hamanaka RB, et al. Metformin inhibits mitochondrial complex I of cancer cells to reduce tumorigenesis. Elife (2014). PMID: 24843020 DOI: 10.7554/eLife.02242 Source material

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