PP-60
PP-60 is an apoptosis inducer. PP-60 inhibits the proliferation of cancer cells and induces cancer cell apoptosis. PP-60 exerts anti-tumor effects in nude mouse liver tumor models. PP-60 is applicable to research related to cancers such as liver cancer, lung cancer, and prostate cancer.
For research use only. We do not sell to patients.
- Formula: C142H252N36O40
- Molecular Weight:3103.74
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
PP-60 (24 h) exhibits potent antiproliferative activity against HepG2, A549 and PC-3 cells, with IC50 values of 1.73, 2.15 and 2.69 μM[1].
PP-60 (2 μM; 2-4 h) exhibits excellent cellular uptake capacity[1].
PP-60 (0-5 μM) inhibits G2 phase cell cycle progression in HepG2 cells in a dose-dependent manner, and the percentage of cells in the G2 phase reaches approximately 35% at a concentration of 5 μM[1].
PP-60 (0-5 μM, 6 h) induces apoptosis in HepG2 cells[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:HepG2 cells
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Concentration:2 μM
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Incubation Time:2, 4 h
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Result:Increased FITC fluorescence signal intensity indicates a stronger cellular uptake capacity.
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Cell Line:HepG2 cells
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Concentration:0, 1, 2, 5 μM
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Incubation Time:6 h
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Result:Induced apoptosis, at a concentration of 5 μM, the apoptosis rate is approximately 80%.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female; HepG2 (2 × 106 cells/mouse) xenograft model)[1]
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Dosage:0.5 mg per mouse
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Administration:intratumoral injection; on day 1, 6, and 15
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Result:Exhibited potent antitumor activity.
Reduced tumor volume; decreased tumor weight; showed the highest caspase 3 positive staining; reduced Ki67 positive cells to the lowest level; induced significant tumor cell apoptosis.
Chemical Information
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Molecular Weight 3103.74
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Formula C142H252N36O40
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Sequence
Ac-{Arg(β-Glu(1→4)-α-Glu)}-Leu-{(S)-2-(4-pentenyl)alanine}-Lys-Asp-Lys-{(S)-2-(4-pentenyl)alanine}-Lys-Gly-Ile-Gly-Lys-Leu-Ala-Gly-Lys-Ala-Ala-Leu-Gly-Ala-{(S)-2-(4-pentenyl)alanine}--Lys-Thr-Leu-{(S)-2-(4-pentenyl)alanine}-NH2 (RCM bridge: {S5}3-{S5}7, {S5}22-{S5}26)
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Sequence Shortening
Ac-{Arg(β-Glu(1→4)-α-Glu)}-L-{S5}-KDK-{S5}-KGIGKLAGKAALGA-{S5}-KTL-{S5}-NH2 (RCM bridge: {S5}3-{S5}7, {S5}22-{S5}26)
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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.
Protocols
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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
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Liver Cancer Modeling
Liver cancer can be classified into primary liver cancer and secondary liver cancer. Secondary liver cancer is the metastatic liver cancer. Primary liver cancer includes hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma (ICC) and fibrolamellar HCC, of which HCC is the most common form, accounting for approximately 90% of primary liver cancers[1]. HCC mouse models include chemical agent-induced models, transplanted tumor models, and genetic engineered models.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)