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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- Formule: C41H52N8O3
- Masse moléculaire:704.90
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
In Vitro
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. Further protocols information, click here.
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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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Masse moléculaire 704.90
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Formule 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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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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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FRC-303 Related Classifications
HY-183602 Related Classifications
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