1. NF-κB
  2. NF-κB
  3. 4-Hydroxychalcone

4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice.

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4-Hydroxychalcone Chemical Structure

4-Hydroxychalcone Chemical Structure

CAS No. : 20426-12-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity[1]. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice[2].

IC50 & Target

NF-κB[2]

Cellular Effect
Cell Line Type Value Description References
A549 IC50
> 20 μM
Compound: 9e
Inhibition of TNFalpha induced NF-kappaB activation in human A549 cells by luciferase reporter gene assay
Inhibition of TNFalpha induced NF-kappaB activation in human A549 cells by luciferase reporter gene assay
[PMID: 19883086]
DLD-1 EC50
51 μM
Compound: 8
Cytotoxicity against human DLD-1 cells assessed as reduction in cell viability incubated for 48 hrs by AlamarBlue-based assay
Cytotoxicity against human DLD-1 cells assessed as reduction in cell viability incubated for 48 hrs by AlamarBlue-based assay
[PMID: 36356534]
FHC CC50
> 100 μM
Compound: 8
Cytotoxicity against human FHC cells assessed as reduction in cell viability incubated for 48 hrs by AlamarBlue-based assay
Cytotoxicity against human FHC cells assessed as reduction in cell viability incubated for 48 hrs by AlamarBlue-based assay
[PMID: 36356534]
HCT-116 EC50
32 μM
Compound: 8
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by AlamarBlue-based assay
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by AlamarBlue-based assay
[PMID: 36356534]
HCT-116 EC50
32 μM
Compound: 8
Cytotoxicity against p53-/- human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by AlamarBlue-based assay
Cytotoxicity against p53-/- human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by AlamarBlue-based assay
[PMID: 36356534]
HT-29 IC50
24.6 μM
Compound: 16
Cytotoxicity against Homo sapiens (human) HT-29 cells after 72 hr by MTT assay
Cytotoxicity against Homo sapiens (human) HT-29 cells after 72 hr by MTT assay
10.1007/s00044-011-9549-9
HT-29 EC50
39 μM
Compound: 8
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by AlamarBlue-based assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by AlamarBlue-based assay
[PMID: 36356534]
K562 IC50
24 μM
Compound: 4-Hydroxychalcone
Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay
Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay
[PMID: 24775915]
Neutrophil IC50
11.6 μM
Compound: 25
Inhibition of PMA-induce ROS/RNS generation in human neutrophils measured up to 30 mins in presence of 30 mM glucose by luminol-amplified chemiluminescence method
Inhibition of PMA-induce ROS/RNS generation in human neutrophils measured up to 30 mins in presence of 30 mM glucose by luminol-amplified chemiluminescence method
[PMID: 33006891]
Neutrophil IC50
8.8 μM
Compound: 25
Inhibition of PMA-induce ROS/RNS generation in human neutrophils measured up to 30 mins in presence of 5.5 mM glucose by luminol-amplified chemiluminescence method
Inhibition of PMA-induce ROS/RNS generation in human neutrophils measured up to 30 mins in presence of 5.5 mM glucose by luminol-amplified chemiluminescence method
[PMID: 33006891]
NIH3T3 IC50
> 20 μM
Compound: 1i
Inhibition of cobalt chloride-induced HIF-1 activation expressed in mouse NIH3T3 cells after 8 hrs by luciferase reporter gene assay
Inhibition of cobalt chloride-induced HIF-1 activation expressed in mouse NIH3T3 cells after 8 hrs by luciferase reporter gene assay
[PMID: 21112783]
SGC-7901 IC50
13.74 μM
Compound: 16
Cytotoxicity against Homo sapiens (human) SGC7901 cells after 72 hr by MTT assay
Cytotoxicity against Homo sapiens (human) SGC7901 cells after 72 hr by MTT assay
10.1007/s00044-011-9549-9
Molecular Weight

224.25

Formula

C15H12O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=CC=C1)/C=C/C2=CC=C(O)C=C2

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 : ≥ 250 mg/mL (1114.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.4593 mL 22.2965 mL 44.5931 mL
5 mM 0.8919 mL 4.4593 mL 8.9186 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

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (9.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (9.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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 4.4593 mL 22.2965 mL 44.5931 mL 111.4827 mL
5 mM 0.8919 mL 4.4593 mL 8.9186 mL 22.2965 mL
10 mM 0.4459 mL 2.2297 mL 4.4593 mL 11.1483 mL
15 mM 0.2973 mL 1.4864 mL 2.9729 mL 7.4322 mL
20 mM 0.2230 mL 1.1148 mL 2.2297 mL 5.5741 mL
25 mM 0.1784 mL 0.8919 mL 1.7837 mL 4.4593 mL
30 mM 0.1486 mL 0.7432 mL 1.4864 mL 3.7161 mL
40 mM 0.1115 mL 0.5574 mL 1.1148 mL 2.7871 mL
50 mM 0.0892 mL 0.4459 mL 0.8919 mL 2.2297 mL
60 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8580 mL
80 mM 0.0557 mL 0.2787 mL 0.5574 mL 1.3935 mL
100 mM 0.0446 mL 0.2230 mL 0.4459 mL 1.1148 mL
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Help & FAQs
  • 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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4-Hydroxychalcone
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