2'-Hydroxy-4-methoxychalcone
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2'-Hydroxy-4-methoxychalcone is a PPARγ agonist. 2'-Hydroxy-4-methoxychalcone also exhibits inhibitory activity against gelatinase/collagenase and human glutathione S-transferase (GST), with an IC50 of 5.2 μM and a Ki of 15.36 μM against GST. 2'-Hydroxy-4-methoxychalcone inhibits both the NF-κB and AP-1 signaling pathways, exerting anti-inflammatory activity; it also inhibits COX-2, conferring anti-cancer/anti-angiogenic activity. 2'-Hydroxy-4-methoxychalcone can be used in studies related to atherosclerosis, inflammatory diseases and cancer.
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- CAS No.: 3327-24-0
- 화학식: C16H14O3
- 분자량:254.28
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보관:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Biological Activity
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PPARγ |
COX-2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780cisR | GI50 |
15.94 μM
Compound: 2
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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
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[PMID: 24565968] |
| HK-2 | IC50 |
23.7 μM
Compound: 18
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Growth inhibition of HK2 cells by sulforhodamine assay
Growth inhibition of HK2 cells by sulforhodamine assay
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[PMID: 17383189] |
| HL-60 | IC50 |
48.7 μM
Compound: 10
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Cytotoxicity against human HL60 cells by MTT assay
Cytotoxicity against human HL60 cells by MTT assay
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[PMID: 25091929] |
| NALM-6 | IC50 |
50.2 μM
Compound: 10
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Cytotoxicity against human NALM6 cells by MTT assay
Cytotoxicity against human NALM6 cells by MTT assay
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[PMID: 25091929] |
| TK-10 | IC50 |
67 μM
Compound: 18
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Growth inhibition of TK10 cells by sulforhodamine assay
Growth inhibition of TK10 cells by sulforhodamine assay
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[PMID: 17383189] |
| WM-115 | IC50 |
60.5 μM
Compound: 10
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Cytotoxicity against human WM115 cells by MTT assay
Cytotoxicity against human WM115 cells by MTT assay
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[PMID: 25091929] |
2'-Hydroxy-4-methoxychalcone (0.25-1 μM; 24 h) weakly inhibits gelatinase/collagenase activity in a cell-free biochemical assay, with 33.7% inhibition observed at 1 μM[1].
2'-Hydroxy-4-methoxychalcone (1-100 μM; 3 d) potently inhibits CPAE cell proliferation in a concentration-dependent manner with an IC50 of 12.7 μM[1].
2'-Hydroxy-4-methoxychalcone (3-30 μM; 1 hr preincubation + 12 hr incubation with LPS) potently inhibits LPS-induced nitrite production in RAW 264.7 cells, with maximal inhibition observed at 30 μM[3].
2'-Hydroxy-4-methoxychalcone (3-30 μM; 1 hr preincubation + 6 hr incubation with LPS) potently inhibits LPS-induced TNF-α production in RAW 264.7 cells, with maximal inhibition observed at 30 μM[3].
2'-Hydroxy-4-methoxychalcone (3-30 μM; 1 hr preincubation + 12 hr incubation with LPS) inhibits LPS-induced iNOS protein expression in RAW 264.7 cells in a concentration-dependent manner, with near-complete inhibition at 30 μM[3].
2'-Hydroxy-4-methoxychalcone (10-30 μM; 1 hr preincubation + 4 hr incubation with LPS) suppresses LPS-induced TNF-α mRNA expression in RAW 264.7 cells, with maximal suppression at 30 μM[3].
2'-Hydroxy-4-methoxychalcone (3-30 μM; 1 hr preincubation + 1 hr incubation with LPS) inhibits LPS-induced NF-κB activation in RAW 264.7 cells in a concentration-dependent manner[3].
2'-Hydroxy-4-methoxychalcone (3-30 μM; 1 hr preincubation + 1 hr incubation with LPS) inhibits LPS-induced AP-1 activation in RAW 264.7 cells in a concentration-dependent manner[3].
2'-Hydroxy-4-methoxychalcone (3-30 μM; 1 hr preincubation + 20 min incubation with LPS) inhibits LPS-induced IκB-α degradation in RAW 264.7 cells in a concentration-dependent manner[3].
2'-Hydroxy-4-methoxychalcone (3-30 μM; 1 hr preincubation + 30 min incubation with LPS) inhibits LPS-induced JNK phosphorylation in RAW 264.7 cells in vitro in a concentration-dependent manner, with maximal inhibition at 30 μM[3].
2'-Hydroxy-4-methoxychalcone (3-30 μM; 1 hr preincubation + 30 min incubation with LPS) inhibits LPS-induced c-jun phosphorylation in RAW 264.7 cells in vitro in a concentration-dependent manner, with maximal inhibition at 30 μM[3].
2'-Hydroxy-4-methoxychalcone (3.93-19.65 μM) noncompetitively inhibits purified human erythrocyte GST with an IC50 of 15.2 μM and a Ki of 15.36 μM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Calf Pulmonary Arterial Endothelial (CPAE) cells
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Concentration:1 μM, 10 μM, 50 μM, 100 μM
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Incubation Time:3 d
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Result:Significantly inhibited CPAE cell proliferation in a concentration-dependent manner, with 96.3% inhibition at 100 μM.
Showed 55.2% inhibition at 50 μM.
Showed 33.3% inhibition at 10 μM.
Showed 24.0% inhibition at 1 μM.
Had an IC50 value of 12.7 μM for the anti-proliferative effect.
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Cell Line:RAW 264.7
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Concentration:3 μM, 10 μM, 30 μM
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Incubation Time:1 hr preincubation + 6 hr incubation with LPS
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Result:Reduced LPS-induced TNF-α levels from 208 pg/mL to 55.0 pg/mL at 30 μM.
Suppressed LPS-induced TNF-α production in a concentration-dependent manner across all tested concentrations.
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Cell Line:RAW 264.7
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Concentration:3 μM, 10 μM, 30 μM
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Incubation Time:1 hr preincubation + 12 hr incubation with LPS
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Result:Suppressed LPS-induced iNOS expression in a concentration-dependent manner, reducing the density ratio to ~0.7 at 3 μM, ~0.6 at 10 μM, and ~0.1 at 30 μM.
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Cell Line:RAW 264.7
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Concentration:10 μM, 30 μM
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Incubation Time:1 hr preincubation + 4 hr incubation with LPS
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Result:Reduced LPS-induced TNF-α mRNA density ratio to ~0.6 at 10 μM and ~0.1 at 30 μM.
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Cell Line:RAW 264.7
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Concentration:3 μM, 10 μM, 30 μM
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Incubation Time:1 hr preincubation + 20 min incubation with LPS
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Result:Inhibited LPS-induced IkB-α degradation in a concentration-dependent manner, increasing the density ratio to ~0.5 at 3 μM, ~0.6 at 10 μM, and ~0.8 at 30 μM.
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Cell Line:RAW 264.7
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Concentration:3 μM, 10 μM, 30 μM
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Incubation Time:1 hr preincubation + 30 min incubation with LPS
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Result:Suppressed LPS-induced JNK phosphorylation in a concentration-dependent manner, reducing the density ratio to ~0.6 at 3 μM, ~0.5 at 10 μM, and ~0.2 at 30 μM.\nSuppressed LPS-induced c-jun phosphorylation in a concentration-dependent manner, reducing the density ratio to ~0.6 at 3 μM, ~0.4 at 10 μM, and ~0.2 at 30 μM.
2'-Hydroxy-4-methoxychalcone (50 μg/mL; subcutaneous injection; single dose) inhibits bFGF-induced angiogenesis in the mouse Matrigel plug assay, reducing hemoglobin content (a marker of functional vasculature) to 6.8 g/dl[1].
2'-Hydroxy-4-methoxychalcone (30 mg/kg; subcutaneous injection; once daily; 20 consecutive days) inhibits primary Lewis lung carcinoma growth in C57BL/6 mice, reducing tumor volume by 27.2%[1].
2'-Hydroxy-4-methoxychalcone (30 mg/kg; intraperitoneal injection; once daily; 10 consecutive days) inhibits sarcoma 180 tumor growth in ICR mice, reducing tumor weight by 33.7%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Chick embryos[1]
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Dosage:30 mg/egg
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Administration:topical application; single dose
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Result:Caused a significant suppression of embryonic angiogenesis, with a 68.4% inhibition rate.
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Animal Model:C57BL/6 (pathogen-free, acclimated for ≥1 week, housed under controlled conditions)[1]
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Dosage:50 μg/mL
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Administration:subcutaneous injection; single dose
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Result:Significantly decreased the bFGF-elevated hemoglobin level from 11.1 g/dl to 6.8 g/dl.
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Animal Model:C57BL/6 (pathogen-free, acclimated for ≥1 week, housed under controlled conditions)[1]
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Dosage:30 mg/kg
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Administration:subcutaneous injection; once daily; 20 consecutive days
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Result:Caused a gradual decrease in tumor growth over the 20-day period; at study end, reduced tumor volume by 27.2% compared to control mice.
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Animal Model:ICR (pathogen-free, acclimated for ≥1 week, housed under controlled conditions)[1]
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Dosage:30 mg/kg
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Administration:intraperitoneal injection; once daily; 10 consecutive days
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Result:Reduced average tumor weight by 33.7% compared to control mice (control average tumor weight: 7.1 g).
Chemical Information
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CAS No. 3327-24-0
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Appearance Solid
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분자량 254.28
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화학식 C16H14O3
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SMILES
O=C(C1=CC=CC=C1O)/C=C/C2=CC=C(OC)C=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
순도&문서
References
[1]. Lee YS, et al. Anti-angiogenic and anti-tumor activities of 2'-hydroxy-4'-methoxychalcone. Biological & pharmaceutical bulletin. 2006 May;29(5):1028-31. [Content Brief]
[2]. Liu CS, et al. 2-hydroxy-4'-methoxychalcone inhibits proliferation and inflammation of human aortic smooth muscle cells by increasing the expression of peroxisome proliferator-activated receptor gamma. Journal of cardiovascular pharmacology. 2012 Apr;59(4):339-51. [Content Brief]
[3]. Ban HS, et al. Inhibition of lipopolysaccharide-induced expression of inducible nitric oxide synthase and tumor necrosis factor-alpha by 2'-hydroxychalcone derivatives in RAW 264.7 cells. Biochemical pharmacology. 2004 Apr 15;67(8):1549-57. [Content Brief]
[4]. Özaslan MS, et al. Evaluation of chalcones as inhibitors of glutathione S-transferase. Journal of biochemical and molecular toxicology. 2018 May;32(5):e22047. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
2'-Hydroxy-4-methoxychalcone Related Classifications
HY-133997 Related Classifications
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