2,6-Didehydropeperomin B
2,6-Didehydropeperomin B is an Ecolignan-type compound and covalent, selective CPT1A inhibitor with a Kd of 1.62 μM. 2,6-Didehydropeperomin B can be isolated from the plant Peperomia dindygulensis. 2,6-Didehydropeperomin B covalently binds to Cys96 of CPT1A, blocks FAO, and disrupts the mitochondrial CPT1A-VDAC1 interaction. 2,6-Didehydropeperomin B triggers Apoptosis. 2,6-Didehydropeperomin B exhibits anti-CRC activity.
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- CAS. Nr.: 1186292-00-1
- Formel: C23H24O8
- Molecular Weight:428.43
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Speicherung:
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Biologische Aktivität
Beschreibung
IC50 & Target
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CPT-1A |
In Vitro
2,6-Didehydropeperomin B (DHP-B) potently inhibits the proliferation of CRC cell lines SW620, LS513, HCT116, RKO, LS180 with IC50 values ranging from 1.8 to 6.8 μM, and shows low toxicity to normal human colon epithelial NCM460 cells with an IC50 of 97.1 μM[1].
2,6-Didehydropeperomin B (4-12 μM; up to 12 days) at concentrations ≥4 μM inhibits 3D spheroid growth of SW620 and LS513 CRC cells over 12 days, and 2,6-Didehydropeperomin B (5 μM; 6 days) reduces proliferation of SW620 and LS180 spheroids, as shown by decreased Ki-67-positive cell percentages after 6 days of treatment[1].
2,6-Didehydropeperomin B binds to wild-type CPT1A with high affinity Kd = 1.62 μM, and the Cys96 residue is essential for this binding interaction[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW620, LS513, HCT116, RKO, LS180
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Concentration:5 μM (multi-cell line testing); 5-10 μM (SW620 dose-response testing)
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Incubation Time:24 h
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Result:Induced apoptosis in all tested CRC cell lines at 5 μM for 24 h, with SW620 cells showing an apoptosis rate of over 50%.
Induced apoptosis in SW620 cells in a dose-dependent manner, with significantly higher apoptosis rates at 5 and 10 μM compared to control.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-PrkdcscidIl2rgem1/Smoc (NSG) (8-12 weeks old)[1]
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Dosage:25 mg/kg
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Administration:intraperitoneal injection; every other day for 14 days
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Result:Significantly reduced rectal tumor weight compared to vehicle control.
Significantly decreased the percentage of Ki-67-positive (proliferative) cells in tumor tissues.
Prolonged median mouse survival to >60 days (compared to 36 days in vehicle controls).
Increased Oil Red O staining in tumor sections, indicating fatty acid accumulation due to inhibited fatty acid oxidation.
Chemical Information
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CAS. Nr. 1186292-00-1
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Molecular Weight 428.43
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Formel C23H24O8
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SMILES
COC1=C(OCO2)C2=CC([C@@H]([C@@]3([H])C(C(OC3)=O)=C)C4=CC(OC)=C(C(OC)=C4)OC)=C1
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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
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Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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