1. Cell Cycle/DNA Damage Epigenetics Apoptosis Cytoskeleton
  2. PARP Apoptosis Microtubule/Tubulin
  3. 2'-Nitroflavone

2'-Nitroflavone is a PARP1 inhibitor. 2'-Nitroflavone inhibits the proliferation, induces cell cycle arrest and apoptosis of triple-negative breast cancer cells. 2'-Nitroflavone also inhibits the migration of triple-negative breast cancer cells and endothelial cells. 2'-Nitroflavone exhibits antitumor activity and can be used in the research of tumors such as triple-negative breast cancer.

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

2'-Nitroflavone

2'-Nitroflavone Chemical Structure

CAS No. : 53277-26-2

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Description

2'-Nitroflavone is a PARP1 inhibitor. 2'-Nitroflavone inhibits the proliferation, induces cell cycle arrest and apoptosis of triple-negative breast cancer cells. 2'-Nitroflavone also inhibits the migration of triple-negative breast cancer cells and endothelial cells. 2'-Nitroflavone exhibits antitumor activity and can be used in the research of tumors such as triple-negative breast cancer[1].

IC50 & Target[1]

PARP1

 

Cellular Effect
Cell Line Type Value Description References
WISH IC50
3 μM
Compound: 14
In vitro inhibitory activity against the growth of WISH cell derived from human cervical carcinoma was determined
In vitro inhibitory activity against the growth of WISH cell derived from human cervical carcinoma was determined
[PMID: 14684314]
In Vitro

2'-Nitroflavone (1.25-40 μM; 0-96 h) inhibits the viability of three triple-negative breast cancer (TNBC) cell lines, MDA-MB-231, BT-549 and MDA-MB-468, with IC50 values of 4.0 μM, 9.2 μM and 6.5 μM after 72 h of treatment, respectively and has IC50 against EA.hy926 endothelial cells of 14.5 μM at 96 h[1].
2'-Nitroflavone (0-25 μM; 72-144 h) inhibits colony formation and migration of triple-negative breast cancer cells, and induces cell cycle arrest and apoptosis[1].
2'-Nitroflavone (1-25 μM; 72 h) reduces the protein level of α-tubulin in MDA-MB-231 and BT-549 cells, disrupts the arrangement of α-tubulin in cells, and induces the formation of multipolar mitotic spindles[1].

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

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231
Concentration: 5 μM
Incubation Time: 72 h
Result: Induced S and G2/M arrest in MDA-MB-231 cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231
Concentration: 1, 5, 25 μM
Incubation Time: 72 h
Result: Significantly decreased viable cells and increased the percentage of early apoptotic cells at 25 μM compared to vehicle.
Significantly increased the percentage of hypodiploid cells at 5 and 25 μM compared to vehicle.

Western Blot Analysis[1]

Cell Line: MDA-MB-231, BT-549
Concentration: 1, 5, 25 μM
Incubation Time: 72 h
Result: Significantly decreased α-tubulin protein expression in both cell lines at 25 μM.
Did not affect actin protein levels at any concentration tested.
In Vivo

2'-Nitroflavone (20 mg/kg; i.p.; 5 times per week for 2 consecutive weeks) exhibits anti-tumor activity in the 4T1 triple-negative breast cancer mouse model[1].

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

Animal Model: BALB/c (female, 6-8 weeks old, 20-25 g, orthotopic syngeneic 4T1 cell model)[1]
Dosage: 20 mg/kg
Administration: i.p.; daily 5 times per week; 2 weeks
Result: Significantly decreased relative tumor volume compared to vehicle controls.
Had significant differences in body, liver, spleen, heart, or kidney weight between groups.
Molecular Weight

267.24

Formula

C15H9NO4

CAS No.
SMILES

O=C1C2=CC=CC=C2OC(C3=C([N+]([O-])=O)C=CC=C3)=C1

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Storage

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

Purity & Documentation
References
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    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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2'-Nitroflavone
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HY-181068
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