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.
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- CAS 番号: 1186292-00-1
- 分子式: C23H24O8
- 分子量:428.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
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CPT-1A |
体外実験
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. Further protocols information, click here.
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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.
体内実験
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.
化学情報
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CAS 番号 1186292-00-1
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分子量 428.43
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)