POLRMT-IN-4
POLRMT-IN-4 is a photoactivated mitochondrial RNA polymerase (POLRMT) inhibitor. POLRMT-IN-4 can be liberated from the photoactivatable prodrug upon irradiation, enables spatiotemporally precise inhibition and localized tissue selectivity. POLRMT-IN-4 disrupts mitochondrial transcription, impairs oxidative phosphorylation, and suppresses cancer cell proliferation. POLRMT-IN-4 can be used in research on various cancers, such as pancreatic cancer.
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- Fòrmula: C23H23FN2O4
- Peso molecular:410.44
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
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RNA Polymerase |
In Vitro
POLRMT-IN-4 (LJ03) (168 h) inhibits the proliferation of MIA PaCa-2 pancreatic cancer cells with an IC50 of 0.127 μM and HEK293T normal cells with an IC50 of 0.327 μM[1].
POLRMT-IN-4 (LJ03) (500 nM; 12 h) reduces the mitochondrial ND1 transcript level in MIA PaCa-2 cells to 22.2% of control and in HEK293T cells to 39.9% of control[1].
POLRMT-IN-4 (LJ03) (25-100 nM; 14 days) significantly suppresses colony formation of MIA PaCa-2 cells[1].
POLRMT-IN-4 (LJ03) (500 nM; 96 h) does not perturb cell cycle progression in MIA PaCa-2 cells[1].
POLRMT-IN-4 (LJ03) (500 nM; 96 h) does not trigger apoptotic pathways in MIA PaCa-2 cells[1].
POLRMT-IN-4 (LJ03) (168 h) exhibits broad-spectrum antiproliferative activity against multiple cancer cell lines (A2780, HeLa, A431, MDA-MB-468, HepG2) with activity unaffected by irradiation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MIA PaCa-2 cells
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Concentration:500 nM
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Incubation Time:96 h
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Result:Did not cause significant changes in the distribution of MIA PaCa-2 cells across G1, S, and G2 phases after 96 h of incubation in the dark or upon light irradiation.
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Cell Line:MIA PaCa-2 cells
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Concentration:500 nM
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Incubation Time:96 h
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Result:Did not induce significant early or late apoptotic markers in MIA PaCa-2 cells after 96 h of incubation in the dark or upon light irradiation.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Zebrafish (Danio rerio, AB strain) bearing MIA PaCa-2 cells.[1]
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Dosage:500 nM
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Administration:Aqueous exposure; 3 days
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Result:Significantly suppressed tumor-associated fluorescence intensity.
Chemical Information
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Peso molecular 410.44
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Fòrmula C23H23FN2O4
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SMILES
O=C1C=C(C2=CC=CC=C2C)C3=C(O1)C=C(O[C@H](C)C(N4CCNCC4)=O)C(F)=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
POLRMT-IN-4 Related Classifications
HY-181072 Related Classifications
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