FRC-303
FRC-303 is a CHD1 inhibitor with a Kd of 0.14 μM and an IC50 of 0.18 μM. FRC-303 binds to the H3K4me3 binding site of CHD1 tandem chromodomain, forms aromatic cage interactions and extended ligand contacts, acts as a methyl-lysine mimic, and occupies natural peptide ligand-binding regions. FRC-303 can be used for the research of prostate cancer.
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- Fòrmula: C41H52N8O3
- Peso molecular:704.90
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
FRC-303 (Compound 2s) binds to purified recombinant CHD1 tandem chromodomain with a Kd of 0.14 μM[1].
FRC-303 inhibits the interaction between purified recombinant CHD1 tandem chromodomain and H3K4me3 peptide in a TR-FRET assay with an IC50 of 0.18 μM[1].
FRC-303 engages exogenous CHD1 tandem chromodomain in transfected HEK293T cells with an EC50 of 15 μM in a NanoBRET assay[1].
FRC-303 (25-100 μM) dose-dependently inhibits binding of endogenous CHD1 to LSD1-K114me3 peptide in HEK293T cell lysates[1].
FRC-303 (10 μM) does not inhibit the catalytic activity of purified LSD1, KMT9, METTL21A, EHMT2 (G9a), SET8, or NSD2 enzymes[1].
FRC-303 (16 μM) does not inhibit H3K4me3 peptide binding to purified TAF3, SPIN1, or PHF8 reader domains[1].
FRC-303 (0.8-6 μM; 48 h) impairs viability of PC-3M-Luc prostate cancer cells, with viability reduced to ~5% at 6 μM[1].
FRC-303 (0.8-6 μM; 48 h) potently impairs viability of 22Rv1 prostate cancer cells, with viability reduced to ~5% or lower at concentrations ≥2.7 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3M-Luc prostate cancer cells
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Concentration:0.8 μM; 1.2 μM; 1.8 μM; 2.7 μM; 4 μM; 6 μM
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Incubation Time:48 h
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Result:Maintained viability ≥100% at 0.8 μM and 1.2 μM.
Decreased viability to ~115% at 1.8 μM, ~40% at 2.7 μM, ~10% at 4 μM, and ~5% at 6 μM relative to DMSO control.
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Cell Line:22Rv1 prostate cancer cells
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Concentration:0.8 μM; 1.2 μM; 1.8 μM; 2.7 μM; 4 μM; 6 μM
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Incubation Time:48 h
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Result:Maintained viability ~100% at 0.8 μM and ~90% at 1.2 μM.
Decreased viability to ~10% at 1.8 μM, and remained at ~5% or lower at 2.7 μM, 4 μM, and 6 μM relative to DMSO control.
Chemical Information
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Peso molecular 704.90
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Fòrmula C41H52N8O3
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SMILES
COCCN1N=NC(COC2=CC=C(C=C2)CNC3CCN(C4=NC5=CC(OCC)=CC=C5C(NC6CCN(CC7=CC=CC=C7)CC6)=C4)CC3)=C1
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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)
FRC-303 Related Classifications
HY-183602 Related Classifications
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