FRC-222
FRC-222 is a CHD1 tandem chromodomain inhibitor with a Kd of 0.15 μM and an IC50 of 0.18 μM. FRC-222 binds to the H3K4me3 binding site of CHD1 tandem chromodomain via aromatic cage interactions and extended ligand contacts. FRC-222 can be used for the research of prostate cancer[1].
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- Formule: C36H45N5O2
- Masse moléculaire:579.77
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
FRC-222 (Compound 2n) binds to purified recombinant CHD1 tandem chromodomain with a Kd of 0.15 μM[1].
FRC-222 inhibits the interaction between purified recombinant CHD1 tandem chromodomain and H3K4me3 peptide with an IC50 of 0.49 μM[1].
FRC-222 (25-100 μM) engages endogenous full-length CHD1 in HEK293T cell lysate, competitively inhibiting its binding to LSD1-K114me3 peptide in a concentration-dependent manner[1].
FRC-222 (10 μM) shows high selectivity against purified LSD1, KMT9, METTL21A, EHMT2 (G9a), SET8, and NSD2 enzymes, with minimal inhibition of DNMT1[1].
FRC-222 (16 μM) shows high selectivity against purified TAF3, SPIN1, and PHF8 methyl-lysine reader domains, with no significant inhibition of H3K4me3 peptide binding[1].
FRC-222 (0.8-6 μM; 48 h) impairs the viability of PC-3M-Luc prostate cancer cells in a concentration-dependent manner, with significant inhibition observed at concentrations ≥1.8 μM[1].
FRC-222 (0.8-6 μM; 48 h) potently impairs the viability of 22Rv1 prostate cancer cells in a concentration-dependent manner, with significant inhibition observed at concentrations ≥1.8 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:Retained over 110% of control cell viability at 0.8 μM and 1.2 μM.
Reduced viability to 60% of control at 1.8 μM.
Reduced viability to 35% of control at 2.7 μM.
Reduced viability to 25% of control at 4 μM.
Reduced viability to ~5% of control at 6 μM.
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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:Retained over 110% of control cell viability at 0.8 μM.
Retained ~90% of control viability at 1.2 μM.
Reduced viability to ~10% of control at 1.8 μM.
Reduced viability to ≤10% of control at concentrations ≥2.7 μM.
Chemical Information
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Masse moléculaire 579.77
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Formule C36H45N5O2
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SMILES
COC1=CC=C(C=C1)CNC2CCN(C3=NC4=CC(OCC)=CC=C4C(NC5CCN(CC6=CC=CC=C6)CC5)=C3)CC2
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FRC-222 Related Classifications
HY-183603 Related Classifications
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