tP4-CPP12
tP4-CPP12 is a RMI1/2 heterodimer inhibitor with an IC50 of 110 nM. tP4-CPP12 binds competitively at the FANCM-RMI interaction site and disrupts endogenous FANCM-RMI protein-protein interactions. tP4-CPP12 induces antiproliferative effects in ALT-positive osteosarcoma cells. tP4-CPP12 is applicable for the research of ALT-positive osteosarcoma.
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- Formule: C145H199N39O25
- Masse moléculaire:2888.38
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
In Vitro
tP4-CPP12 (6.75-12.5 µM, serial dilutions; 72 h) selectively induces antiproliferative effects in ALT-positive U-2 OS osteosarcoma cells with an IC50 of 8.8 µM, with a more pronounced effect than on telomerase-positive SJSA-1 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:ALT-positive osteosarcoma U-2 OS cells, telomerase-positive osteosarcoma SJSA-1 cells
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Concentration:6.75 and 12.5 µM
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Incubation Time:72 h
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Result:Induced an antiproliferative effect in ALT-positive U-2 OS cells with an IC50 of 8.8 µM.
Reduced U-2 OS cell viability to ~60% at 6.75 µM (compared to ~100% for telomerase-positive SJSA-1 cells).
Reduced U-2 OS cell viability to near 0% at 12.5 µM (compared to ~60% for SJSA-1 cells).
Showed minimal effect on cell viability when using the non-binding control tP4-nb-CPP12 at all tested concentrations.
Chemical Information
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Masse moléculaire 2888.38
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Formule C145H199N39O25
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Sequence
Ac-His-Phe-Lys-Leu-Tyr-Trp-Pro-Pro-Phe-Leu-Gly-Ser-Cyclo(Phe-{d-Phe}-{2-Nal}-Arg-{d-Arg}-Arg-{d-Arg}-Gln) (Disulfide bridge: Phe13-Gln20)
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Sequence Shortening
Ac-HFKLYWPPFLGS-Cyclo(F-{d-Phe}-{2-Nal}-R-{d-Arg}-R-{d-Arg}-Q) (Disulfide bridge: Phe13-Gln20)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Hepatotoxicity Study
This protocol evaluates hepatotoxicity using complementary in vivo mouse APAP acute liver injury and in vitro hepatocyte-based cytotoxicity readouts. In vivo APAP injury is assessed by serum ALT/AST, liver histology, hepatic glutathione, protein adducts, necrosis, inflammation, and regeneration-related endpoints. In vitro hepatotoxicity is assessed by loss of viability, leakage of ALT/AST/LDH, oxidative-stress markers, mitochondrial function, nuclear morphology, intracellular calcium, and high-content imaging endpoints.
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)