2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. 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].

For research use only. We do not sell to patients.

FRC-222

FRC-222 Chemical Structure

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FRC-222 Related Antibodies

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Description

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].

In Vitro

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.

FRC-222 Related Antibodies

Cell Viability Assay[1]

Cell Line: PC-3M-Luc prostate cancer cells
Concentration: 0.8 μM; 1.2 μM; 1.8 μM; 2.7 μM; 4 μM; 6 μM
Incubation Time: 48 h
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.

Cell Viability Assay[1]

Cell Line: 22Rv1 prostate cancer cells
Concentration: 0.8 μM; 1.2 μM; 1.8 μM; 2.7 μM; 4 μM; 6 μM
Incubation Time: 48 h
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.
Molecular Weight

579.77

Formula

C36H45N5O2
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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References
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FRC-222 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FRC-222FRC222FRC 222DNA/RNA Synthesisprostate cancer22Rv1 prostate cancer cellsKMT9CHD1 tandem chromodomainPC-3M-Luc prostate cancer cellsHEK293T cell lysateMETTL21AEHMT2 (G9a)H3K4me3LSD1Inhibitorinhibitorinhibit

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