Petasiphenol
Petasiphenol is a phenolic natural product found in Petasites japonicus, possessing selective inhibitory activity against DNA polymerase λ. Petasiphenol binds to the N-terminal BRCT domain of DNA polymerase λ, with an IC50 of 7.8 μM against DNA polymerase λ. Petasiphenol induces cell growth inhibition, G1 phase cell cycle arrest in human cancer cell lines, and exhibits anti-inflammatory activity against TPA-induced mouse ear inflammation. Petasiphenol can be used for research on cancer and inflammation-related diseases.
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- CAS. Nr.: 145904-50-3
- Formel: C18H16O7
- Molecular Weight:344.32
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Human pol λ 7.6 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NUGC-3 | LD50 |
66 μM
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Growth inhibitory activity against human NUGC-3 gastric cancer cells assessed as reduction in cell survival incubated for 48 hrs by MTT assay.
Growth inhibitory activity against human NUGC-3 gastric cancer cells assessed as reduction in cell survival incubated for 48 hrs by MTT assay.
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14599551 |
| BALL-1 | LD50 |
48 μM
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Growth inhibitory activity against human BALL-1 lymphoblastoid leukemia cells assessed as reduction in cell survival incubated for 48 hrs by MTT assay.
Growth inhibitory activity against human BALL-1 lymphoblastoid leukemia cells assessed as reduction in cell survival incubated for 48 hrs by MTT assay.
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14599551 |
| MOLT-4 | LD50 |
48 μM
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Growth inhibitory activity against human MOLT-4 lymphoblastic leukemia cells assessed as reduction in cell survival incubated for 48 hrs by MTT assay.
Growth inhibitory activity against human MOLT-4 lymphoblastic leukemia cells assessed as reduction in cell survival incubated for 48 hrs by MTT assay.
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14599551 |
In Vitro
Petasiphenol selectively and dose-dependently inhibits human DNA polymerase λ activity with an IC50 of 7.8 µM[1].
Petasiphenol selectively inhibits human DNA polymerase λ (IC50 = 7.6 µM) without affecting other DNA polymerases or metabolic enzymes; it selectively binds to the N-terminal BRCT domain of human DNA polymerase λ, with a Kd of 7.99 µM for the isolated BRCT domain and a Kd of 8.15 µM for the full-length enzyme[1].
Petasiphenol inhibits human DNA polymerase λ in a non-competitive manner with respect to both the DNA template and dNTP substrate, with Ki values of 3.8 µM and 4.5 µM, respectively[1].
Petasiphenol binds to a pocket in the N-terminal BRCT domain of human DNA polymerase λ, interacting primarily through hydrogen bonds with the hydrophilic residues Gln76, Arg93, and Arg99[1].
Petasiphenol (48 h) inhibits the growth of human NUGC-3 gastric cancer cells with an LD50 of 66 μM; it inhibits the growth of human BALL-1 and MOLT-4 leukemia cell lines with LD50 values of approximately 48 μM[2].
Petasiphenol (66 μM; 48 h) arrests human NUGC-3 gastric cancer cells in the G1 phase of the cell cycle[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NUGC-3
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Concentration:66 μM
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Incubation Time:48 h
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Result:Arrested NUGC-3 cells in the G1 phase, increasing the G1 phase population from 43.9% to 58.8% and decreasing the G2/M phase population from 14.3% to 10.0% compared to the control.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 145904-50-3
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Molecular Weight 344.32
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Formel C18H16O7
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SMILES
O=C(OCC(=O)CC1=CC=C(O)C(O)=C1)C=CC2=CC=C(O)C(O)=C2
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Petasiphenol Related Classifications
HY-N21777 Related Classifications
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