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Art. -Nr.: HY-161027

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2,6-Didehydropeperomin B

DHP-B is an Ecolignan-type compound and covalent, selective CPT1A inhibitor with a K_d 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.

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CAS. Nr.: 1186292-00-1
Formel: C₂₃H₂₄O₈
Molecular Weight:428.43

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (280 KB)

2,6-Didehydropeperomin B Chemical Structure

CAS. Nr.: 1186292-00-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

CPT-1A

In Vitro

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 K_i-67-positive cell percentages after 6 days of treatment^[1].
DHP-B binds to wild-type CPT1A with high affinity K_d = 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.

Apoptosis Analysis^[1]

Cell Line:

SW620, LS513, HCT116, RKO, LS180
Concentration:

5 μM (multi-cell line testing); 5-10 μM (SW620 dose-response testing)
Incubation Time:

24 h
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

DHP-B (25 mg/kg; intraperitoneal injection; every other day for 14 days) significantly suppresses orthotopic colorectal tumor growth, reduces tumor cell proliferation, increases tumor cell apoptosis, inhibits in vivo fatty acid oxidation, and extends median survival of tumor-bearing NSG mice to >60 days^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NOD-PrkdcscidIl2rgem1/Smoc (NSG) (8-12 weeks old)^[1]
Dosage:

25 mg/kg
Administration:

intraperitoneal injection; every other day for 14 days
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

CAS. Nr. 1186292-00-1
Molecular Weight 428.43
Formel C₂₃H₂₄O₈
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hu A, et al. A novel CPT1A covalent inhibitor modulates fatty acid oxidation and CPT1A-VDAC1 axis with therapeutic potential for colorectal cancer. Redox Biol. 2023;68:102959. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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