1. NF-κB Anti-infection Apoptosis Autophagy
  2. NF-κB Fungal Apoptosis Autophagy
  3. 2′-Hydroxychalcone

2′-Hydroxychalcone is a hydroxyl derivative of chalcones with anticancer activities. 2'-Hydroxychalcone inhibits NF-κB pathway and induces autophagy and apoptosis in breast cancer cells. 2′-Hydroxychalcone shows a better antifungal activity against the complex Paracoccidioides spp.

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2′-Hydroxychalcone Chemical Structure

2′-Hydroxychalcone Chemical Structure

CAS No. : 1214-47-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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100 mg In-stock
500 mg In-stock
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Description

2′-Hydroxychalcone is a hydroxyl derivative of chalcones with anticancer activities. 2'-Hydroxychalcone inhibits NF-κB pathway and induces autophagy and apoptosis in breast cancer cells[1]. 2′-Hydroxychalcone shows a better antifungal activity against the complex Paracoccidioides spp[2].

Cellular Effect
Cell Line Type Value Description References
A2780cisR GI50
13.45 μM
Compound: 6
Growth inhibition of cisplatin-resistant human A2780cis cells after 7 days by crystal violet staining based clonogenic assay
Growth inhibition of cisplatin-resistant human A2780cis cells after 7 days by crystal violet staining based clonogenic assay
[PMID: 24565968]
A549 IC50
> 20 μM
Compound: 2
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]
HK-2 IC50
24.4 μM
Compound: 8
Growth inhibition of HK2 cells by sulforhodamine assay
Growth inhibition of HK2 cells by sulforhodamine assay
[PMID: 17383189]
HL-60 IC50
18 μM
Compound: 2
Cytotoxicity against human HL60 cells by MTT assay
Cytotoxicity against human HL60 cells by MTT assay
[PMID: 25091929]
HT-29 IC50
85 μM
Compound: 8
Growth inhibition of HT29 cells by sulforhodamine assay
Growth inhibition of HT29 cells by sulforhodamine assay
[PMID: 17383189]
K562 IC50
60.7 μM
Compound: 1
Cytotoxicity against Homo sapiens (human) K562 cells after 72 hr by MTT assay
Cytotoxicity against Homo sapiens (human) K562 cells after 72 hr by MTT assay
10.1007/s00044-010-9344-z
L929 CC50
79.5 μM
Compound: 1
Cytotoxicity in mouse NCTC-929 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity in mouse NCTC-929 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31000155]
MCF7 IC50
78 μM
Compound: 8
Growth inhibition of MCF7 cells by sulforhodamine assay
Growth inhibition of MCF7 cells by sulforhodamine assay
[PMID: 17383189]
MOLM-13 GI50
> 10 μM
Compound: 1
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 32975953]
MV4-11 GI50
> 10 μM
Compound: 1
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 32975953]
NALM-6 IC50
37.5 μM
Compound: 2
Cytotoxicity against human NALM6 cells by MTT assay
Cytotoxicity against human NALM6 cells by MTT assay
[PMID: 25091929]
PBMC IC50
11 μg/mL
Compound: 15
Immunosuppressive activity in human PBMC assessed as inhibition of PHA-induced T cell proliferation after 72 hrs by [3H]thymidine incorporation assay
Immunosuppressive activity in human PBMC assessed as inhibition of PHA-induced T cell proliferation after 72 hrs by [3H]thymidine incorporation assay
10.1007/s00044-013-0564-x
PBMC IC50
19.7 μg/mL
Compound: 15
Immunosuppressive activity in human PBMC assessed as inhibition of PHA/PMA-induced IL-2 production after 18 hrs by ELISA
Immunosuppressive activity in human PBMC assessed as inhibition of PHA/PMA-induced IL-2 production after 18 hrs by ELISA
10.1007/s00044-013-0564-x
SK-N-MC IC50
61.2 μM
Compound: 1
Cytotoxicity against Homo sapiens (human) SK-N-MC cells after 72 hr by MTT assay
Cytotoxicity against Homo sapiens (human) SK-N-MC cells after 72 hr by MTT assay
10.1007/s00044-010-9344-z
THP-1 GI50
> 10 μM
Compound: 1
Antiproliferative activity against human THP-1 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against human THP-1 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 32975953]
TK-10 IC50
79 μM
Compound: 8
Growth inhibition of TK10 cells by sulforhodamine assay
Growth inhibition of TK10 cells by sulforhodamine assay
[PMID: 17383189]
WM-115 IC50
40.8 μM
Compound: 2
Cytotoxicity against human WM115 cells by MTT assay
Cytotoxicity against human WM115 cells by MTT assay
[PMID: 25091929]
In Vitro

2′-Hydroxychalcone (10-90 μM; 12-72 h) suppresses cell viability in a dose-dependent manner, with IC50 values of 37.74 μM and 34.26 μM for the two breast cancer cell lines MCF-7 and CMT-1211, respectively[1].
2′-Hydroxychalcone (10-30 μM; 24 h) promotes autophagy vesicle accumulation in breast cancer cells[1].
2′-Hydroxychalcone (30 μM; 24 h) induces autophagy-dependent apoptosis in breast cancer cells, and increases cleavage of caspase-3 and PARP[1].
2′-Hydroxychalcone (10-30 μM; 24 h) significantly reduces the expression of p-IκB and p-NF-κBp65, and elevates the levels of p-ERK and p-JNK[1].
2′-Hydroxychalcone (30 μM; 12-24 h) increased the intracellular ROS levels and triggered endoplasmic reticulum stress (ERS) of breast cancer cells[1].

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

Cell Viability Assay[1]

Cell Line: MCF-7 and CMT-1211 cells
Concentration: 10 μM, 20 μM, 30 μM, 40 μM, 50 μM, 60 μM, 70 μM, 80 μM, and 90 μM
Incubation Time: 12 h, 24 h, 36 h, 48 h, 60 h, and 72 h
Result: Suppressed cell viability in a dose-dependent manner.

Cell Autophagy Assay[1]

Cell Line: MCF-7 and CMT-1211 cells
Concentration: 10 μM, 20 μM, 30 μM
Incubation Time: 24 h
Result: Induced autophagy and promoted autophagy flux in breast cancer cells.

Apoptosis Analysis[1]

Cell Line: MCF-7 and CMT-1211 cells
Concentration: 30 μM
Incubation Time: 24 h
Result: Induced autophagy-dependent apoptosis of breast cancer cells.

Western Blot Analysis[1]

Cell Line: MCF-7 and CMT-1211 cells
Concentration: 10 μM, 20 μM, 30 μM
Incubation Time: 24 h
Result: Regulated MAPK/NF-κB signaling pathways and inhibited migration/invasion of breast cancer cells.
In Vivo

2'-Hydroxychalcone (20-60 mg/kg; ip; every 2 days; 3 weeks) could exhibit an antitumor effect in vivo without causing significant toxicity to essential organs[1].

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

Animal Model: Five-week-old Balb/C female mice injected with CMT-1211 cells[1]
Dosage: 20 mg/kg, 40 mg/kg, 60 mg/kg
Administration: Intraperitoneal injection; every 2 days; 3 weeks
Result: Suppressed tumor growth and metastasis in vivo.
Molecular Weight

224.25

Formula

C15H12O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (891.86 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 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. 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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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 97.45%

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. 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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Product Name:
2′-Hydroxychalcone
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HY-W012349
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