2,6-Didehydropeperomin B
DHP-B is an Ecolignan-type compound and covalent, selective CPT1A inhibitor with a Kd of 1.62 μM. DHP-B can be isolated from the plant Peperomia dindygulensis. DHP-B covalently binds to Cys96 of CPT1A, blocks FAO, and disrupts the mitochondrial CPT1A-VDAC1 interaction. DHP-B triggers Apoptosis. DHP-B exhibits anti-CRC activity.
For research use only. We do not sell to patients.
- CAS No.: 1186292-00-1
- Formula: C23H24O8
- Molecular Weight:428.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CPT-1A |
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].
DHP-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 DHP-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].
DHP-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.
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 No. 1186292-00-1
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Molecular Weight 428.43
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
2,6-Didehydropeperomin B Related Classifications
HY-161027 Related Classifications
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