Faradiol
Faradiol is a STAT3 inhibitor. Faradiol exerts anti-inflammatory activity by reducing STAT3 phosphorylation in a concentration-dependent manner and inhibiting LPS-induced IL-6 release from human monocytes, while also exhibiting cytotoxicity against leukemia and non-small cell lung cancer cells. Faradiol can be used in research on leukemia, edema, cancer, non-small cell lung cancer, Phorbol 12-myristate 13-acetate (TPA) (HY-18739)-induced inflammation, and skin tumors.
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- No. CAS: 20554-95-4
- Fòrmula: C30H50O2
- Peso molecular:442.72
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Descripciòn
IC50 & Target
[2]|
STAT3 |
IL-6 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NB-4 | IC50 |
32.47 μM
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Cytotoxicity against human NB4 cells assessed as 50% loss of metabolic activity after 24 hrs by MTT assay.
Cytotoxicity against human NB4 cells assessed as 50% loss of metabolic activity after 24 hrs by MTT assay.
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20981868 |
| NB-4 | IC50 |
30.60 μM
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Cytotoxicity against human NB4 cells assessed as 50% loss of metabolic activity after 48 hrs by MTT assay.
Cytotoxicity against human NB4 cells assessed as 50% loss of metabolic activity after 48 hrs by MTT assay.
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20981868 |
| K562 | IC50 |
132.80 μM
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Cytotoxicity against human K562 cells assessed as 50% loss of metabolic activity after 24 hrs by MTT assay.
Cytotoxicity against human K562 cells assessed as 50% loss of metabolic activity after 24 hrs by MTT assay.
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20981868 |
| K562 | IC50 |
60.15 μM
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Cytotoxicity against human K562 cells assessed as 50% loss of metabolic activity after 48 hrs by MTT assay.
Cytotoxicity against human K562 cells assessed as 50% loss of metabolic activity after 48 hrs by MTT assay.
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20981868 |
| CCRF-CEM | GI50 |
3.2 μM
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Antiproliferative activity against human CCRF-CEM leukemia cells assessed as growth inhibition after 48 hrs continuous exposure by sulforhodamine B protein assay.
Antiproliferative activity against human CCRF-CEM leukemia cells assessed as growth inhibition after 48 hrs continuous exposure by sulforhodamine B protein assay.
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11809525 |
| SR | GI50 |
3.5 μM
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Antiproliferative activity against human SR leukemia cells assessed as growth inhibition after 48 hrs continuous exposure by sulforhodamine B protein assay.
Antiproliferative activity against human SR leukemia cells assessed as growth inhibition after 48 hrs continuous exposure by sulforhodamine B protein assay.
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11809525 |
| EKVX | GI50 |
2.2 μM
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Antiproliferative activity against human EKVX non-small cell lung cancer cells assessed as growth inhibition after 48 hrs continuous exposure by sulforhodamine B protein assay.
Antiproliferative activity against human EKVX non-small cell lung cancer cells assessed as growth inhibition after 48 hrs continuous exposure by sulforhodamine B protein assay.
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11809525 |
In Vitro
Faradiol (10-4 M; 48 h) exhibits selective cytotoxicity against CCRF-CEM, K-582, SR, and EKVX human cancer cell lines, with GI50 values of 2.2-4.2 µM, and shows moderate cytotoxicity against the remaining tested NCI 60 cell lines (GI50, 10.5-86.9 µM)[6].
Faradiol (20 μM) reduces STAT3 phosphorylation in THP-1 monocytes without affecting NF-κB p65 phosphorylation[1].
Faradiol (20 µM; 30 min-24 h) inhibits LPS-induced IL-6 release in THP-1 human monocytes by 59%[2].
Faradiol (20 µM) reduces STAT3 phosphorylation but not NF-κB p65 phosphorylation in THP-1 human monocytes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human leukemic cell lines NB4 and K562
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Concentration:25 mM (stock); 100 μM (assay starting concentration; seven two-fold serial dilutions)
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Incubation Time:24 h and 48 h
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Result:IC50 values were 32.47 μM (NB4, 24 h), 30.60 μM (NB4, 48 h), 132.80 μM (K562, 24 h), and 60.15 μM (K562, 48 h).
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Cell Line:NCI 60 human cancer cell lines (lung, colon, melanoma, renal, ovarian, brain, and leukemia)
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Concentration:10-4 M starting; five concentrations at ten-fold dilutions
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Incubation Time:48 h
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Result:Exhibited marked cytotoxicity against leukemia cell lines CCRF-CEM (GI50, 3.2 µM), K-582 (GI50, 4.2 µM), and SR (GI50, 3.5 µM), and against non-small cell lung cancer EKVX (GI50, 2.2 µM).
Showed moderate activity against the other cells (GI50, 10.5-86.9 µM).
In Vivo
Faradiol (compound 9) (1 mg/ear; topical administration; single dose; 30 min before TPA) inhibits TPA-induced ear edema in ICR mice, with an ID50 of 0.2 mg/ear[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Albino Swiss (male, 28-30 g, Charles Rivers, Calco, Italy)[5]
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Dosage:120 µg/cm2 (0.27 µmole/cm2)
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Administration:topical; single application; 6 h
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Result:Reduced ear oedema to 2.0 mg, corresponding to 73% inhibition.
Control oedema was 7.4 mg.
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Animal Model:ICR (five mice per group)[9]
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Dosage:1 mg/ear
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Administration:topical; single application; 30 min before TPA
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Result:Inhibited TPA-induced ear edema with an ID50 of 0.2 mg/ear and an inhibitory ratio of 94% at 1 mg/ear.
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Animal Model:ICR (female, 7 weeks old)[10]
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Dosage:0.2 μmol/mouse
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Administration:topical; once 30 min before each TPA application (twice weekly); 20 weeks
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Result:In the DMBA plus TPA plus faradiol group, the first tumor appeared at week 10.
At week 20, 40% of mice were tumor-bearing.
The faradiol group had an average of 2.9 tumors per mouse at week 20.
Faradiol caused a 66% reduction in the average number of tumors per mouse at week 20.
- Kinase activity and phosphorylation assays
- Western Blot
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Cotton Pellet Granuloma
- Carrageenan-Induced Paw Edema
- Research Protocol for Inflammation-related Diseases
- Protocol for Kinase activity and phosphorylation assays
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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No. CAS 20554-95-4
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Peso molecular 442.72
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Fòrmula C30H50O2
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SMILES
CC1(C)[C@@H](O)CC[C@]2(C)[C@@]3([H])CC[C@]4([H])[C@@]5([H])[C@H](C)C(C)=CC[C@@](C)5[C@@H](O)C[C@](C)4[C@@](C)3CC[C@@]12[H]
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Structure Classification
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[8]. Yasukawa K, et al. Inhibitory effect of heliantriol C; a component of edible Chrysanthemum, on tumor promotion by 12-O-tetradecanoylphorbol-13-acetate in two-stage carcinogenesis in mouse skin. Phytomedicine : international journal of phytotherapy and phytopharmacology. 1998 May;5(3):215-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Faradiol Related Classifications
HY-121225 Related Classifications
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