1. Metabolic Enzyme/Protease
  2. Xanthine Oxidase
  3. Broussoflavonol F

Broussoflavonol F is a HER2-RAS-MEK-ERK signaling pathway modulator and mushroom tyrosinase inhibitor, with an IC50 of 82.3 μM against mushroom tyrosinase. Broussoflavonol F reduces the protein expression levels of RAS, HER2, phosphorylated BRAF, phosphorylated MEK and phosphorylated Erk. It induces cell apoptosis, triggers G0/G1 phase cell cycle arrest, and exhibits cytotoxicity against colon cancer cells. Broussoflavonol F is applicable to related research on colon cancer.

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

Broussoflavonol F

Broussoflavonol F Chemical Structure

CAS No. : 162558-94-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Description

Broussoflavonol F is a HER2-RAS-MEK-ERK signaling pathway modulator and mushroom tyrosinase inhibitor, with an IC50 of 82.3 μM against mushroom tyrosinase. Broussoflavonol F reduces the protein expression levels of RAS, HER2, phosphorylated BRAF, phosphorylated MEK and phosphorylated Erk. It induces cell apoptosis, triggers G0/G1 phase cell cycle arrest, and exhibits cytotoxicity against colon cancer cells. Broussoflavonol F is applicable to related research on colon cancer[1].

Cellular Effect
Cell Line Type Value Description References
Hep 3B2 IC50
1.15 μM
Compound: 21
Cytotoxicity against human Hep3B cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
Cytotoxicity against human Hep3B cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
[PMID: 36549116]
HepG2 IC50
30.79 μM
Compound: 21
Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
[PMID: 36549116]
Platelet IC50
16.9 μM
Compound: 16
Antiplatelet activity against rabbit platelets assessed as arachidonic acid-induced platelet aggregation by turbidimetric method
Antiplatelet activity against rabbit platelets assessed as arachidonic acid-induced platelet aggregation by turbidimetric method
[PMID: 8864236]
Platelet IC50
2.7 μM
Compound: 6
Antiplatelet activity against rabbit platelet assessed as inhibition of platelet-activating factor-induced platelet aggregation at 20 uM preincubated 3 mins before PAF challenge by turbidimetric method relative to control
Antiplatelet activity against rabbit platelet assessed as inhibition of platelet-activating factor-induced platelet aggregation at 20 uM preincubated 3 mins before PAF challenge by turbidimetric method relative to control
[PMID: 9358644]
In Vitro

Broussoflavonol F (BFF) (0-20 μM; 24-48 h) exerts selective, concentration- and time-dependent cytotoxicity against HCT-116, LoVo, HT-29, SW480, and colon 26 colon cancer cells, with IC50 values of 6.64 μM (HCT-116) and 7.37 μM (LoVo) after 48 h, and is far less cytotoxic to PBMCs (IC50 = 47 μM)[1].
Broussoflavonol F (BFF) (14.41 μM (HCT-116); 14.50 μM (LoVo); 48 h) significantly suppresses proliferation of HCT-116 and LoVo colon cancer cells when treated at 14.41 μM and 14.50 μM for 48 h, respectively[1].
Broussoflavonol F (BFF) (1.25-7.5 μM (HCT-116); 2.5-10 μM (LoVo); 24-48 h) effectively suppresses colony formation in HCT-116 and LoVo colon cancer cells after 24 h and 48 h treatment, with effects comparable to 5-FU at its IC50 concentrations[1].
Broussoflavonol F (BFF) (1.25-5 μM; 24-48 h) induces G0/G1 phase cell cycle arrest and reduces G2/M phase cell numbers in HCT-116 and LoVo colon cancer cells after 24 h and 48 h treatment[1].
Broussoflavonol F (BFF) (2.5-7.5 μM (HCT-116); 5-10 μM (LoVo); 24-48 h) significantly increases apoptosis in HCT-116 and LoVo colon cancer cells after 24 h and 48 h treatment[1].
Broussoflavonol F (BFF) (1.25-5 μM; 24-48 h) downregulates HER2, RAS, p-BRAF, p-MEK, and p-Erk protein expression (without altering total BRAF, MEK, or Erk) in HCT-116 and LoVo colon cancer cells after 24 h and 48 h treatment, inhibiting the HER2-RAS-MEK-ERK pathway[1].
Broussoflavonol F (BFF) (0-20 μM; 48 h) exhibits cytotoxicity to HMEC-1 cells with an IC50 of 7.1 μM after 48 h treatment[1].
Broussoflavonol F (BFF) (40 μM; 6 h) inhibits tube formation in HMEC-1 cells after 6 h incubation[1].
Broussoflavonol F (BFF) (5 μM; 24 h) reduces cell motility in HMEC-1 cells after 24 h treatment[1].
Broussoflavonol F (multiple concentrations; 20 min) inhibits mushroom tyrosinase using L-tyrosine as substrate with an IC50 of 388.6 μM[2].

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

Cell Proliferation Assay[1]

Cell Line: human colon cancer HCT-116 and LoVo cells
Concentration: 14.41 μM (HCT-116); 14.50 μM (LoVo)
Incubation Time: 48 h
Result: Significantly suppressed cell proliferation in HCT-116 and LoVo cells at the tested concentrations after 48 h.

Cell Proliferation Assay[1]

Cell Line: human colon cancer HCT-116 and LoVo cells
Concentration: 1.25-7.5 μM (HCT-116); 2.5-10 μM (LoVo)
Incubation Time: 24 h; 48 h
Result: Effectively suppressed colony formation in both HCT-116 and LoVo cells after 24 h and 48 h treatment.
Exhibited suppressive effects similar to the positive control 5-FU at 5 μM (HCT-116) and 7.5 μM (LoVo).

Cell Cycle Analysis[1]

Cell Line: human colon cancer HCT-116 and LoVo cells
Concentration: 1.25-5 μM
Incubation Time: 24 h; 48 h
Result: Significantly arrested cells at the G0/G1 phase, accompanied by a decrease in cell number in the G2/M phase in both HCT-116 and LoVo cells after 24 h and 48 h incubation.

Western Blot Analysis[1]

Cell Line: human colon cancer HCT-116 and LoVo cells
Concentration: 1.25-5 μM
Incubation Time: 24 h; 48 h
Result: Significantly decreased the expression levels of HER2, RAS, p-BRAF, p-MEK, and p-Erk in both HCT-116 and LoVo cells after 24 h and 48 h treatment.
Did not regulate the expression levels of total BRAF, MEK, and Erk proteins.
In Vivo

Broussoflavonol F (1.25-5 µM; immersion; continuous; 48 hours) exhibits concentration-dependent anti-angiogenic activity in transgenic Danio rerio embryos, significantly reducing subintestinal vessel length and downregulating key angiogenesis-related genes at 5 µM[1].
Broussoflavonol F (5-10 mg/kg; i.p.; daily; 21 days) at 10 mg/kg suppresses in vivo colon tumor growth, reduces tumor cell proliferation and angiogenesis, and downregulates the HER2-RAS-MEK-ERK pathway in HCT116 xenograft-bearing mice without inducing measurable liver or muscle toxicity[1].

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

Animal Model: Male nude mice (6-8 weeks old, 25-30 g; subcutaneous xenograft of human HCT116 colon cancer cells)[1]
Dosage: 5 mg/kg, 10 mg/kg
Administration: i.p.; daily; 21 days
Result: Significantly reduced final tumor weight relative to control at 10 mg/kg.
Downregulated tumor tissue expressions of RAS, p-BRAF, p-MEK, and p-Erk proteins at 5 mg/kg and 10 mg/kg.
Decreased the number of Ki-67-positive (proliferation) and CD31-positive (angiogenesis) cells in tumor sections at 10 mg/kg.
Caused no significant changes in plasma alanine aminotransferase (ALT), aspartate aminotransferase (AST), creatine kinase (CK), or lactate dehydrogenase (LDH) levels, indicating no obvious liver or muscle toxicity.
Molecular Weight

422.47

Formula

C25H26O6

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(O)=C(C2=CC=C(O)C(C/C=C(C)\C)=C2)OC3=C(C/C=C(C)\C)C(O)=CC(O)=C13

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (236.70 mM; Need ultrasonic; 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 2.3670 mL 11.8352 mL 23.6703 mL
5 mM 0.4734 mL 2.3670 mL 4.7341 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.

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Purity & Documentation

Purity: 98.11%

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 2.3670 mL 11.8352 mL 23.6703 mL 59.1758 mL
5 mM 0.4734 mL 2.3670 mL 4.7341 mL 11.8352 mL
10 mM 0.2367 mL 1.1835 mL 2.3670 mL 5.9176 mL
15 mM 0.1578 mL 0.7890 mL 1.5780 mL 3.9451 mL
20 mM 0.1184 mL 0.5918 mL 1.1835 mL 2.9588 mL
25 mM 0.0947 mL 0.4734 mL 0.9468 mL 2.3670 mL
30 mM 0.0789 mL 0.3945 mL 0.7890 mL 1.9725 mL
40 mM 0.0592 mL 0.2959 mL 0.5918 mL 1.4794 mL
50 mM 0.0473 mL 0.2367 mL 0.4734 mL 1.1835 mL
60 mM 0.0395 mL 0.1973 mL 0.3945 mL 0.9863 mL
80 mM 0.0296 mL 0.1479 mL 0.2959 mL 0.7397 mL
100 mM 0.0237 mL 0.1184 mL 0.2367 mL 0.5918 mL
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Product Name:
Broussoflavonol F
Cat. No.:
HY-N9330
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