2. Epigenetics
  3. DNA Methyltransferase
  4. DNMT1-IN-3

DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor.

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DNMT1-IN-3 Chemical Structure

DNMT1-IN-3 Chemical Structure

CAS No. : 3025012-68-1

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DNMT1-IN-3 Related Antibodies

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Description

DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor[1].

IC50 & Target

DNMT1

0.777 μM (IC50)

In Vitro

DNMT1-IN-3 (compound 7t-S) (0-400 μM; 48 h) demonstrates potential anti-proliferative activity on various tumor cell lines including A2780, HeLa, K562, and SiHa[1].
DNMT1-IN-3 (20-60 μM; 48 h) can arrest K562 cells in the G0 / G1 phase in a concentration-dependent manner, as determined by flow cytometry assays[1].
DNMT1-IN-3 (43.89 μM) can induce apoptosis in K562 cells by upregulating the expression of apoptosis-related genes suppressed by methylation, such as death receptor TRAIL-R2/Dr5 and TNFR-1. TRAIL-R2 can instigate the cell apoptosis signal by recruiting Caspase-8 or Caspase-10 to initiate downstream Caspase cascade reactions. [1]。

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DNMT1-IN-3 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: A2780, HeLa, K562, SiHa cells
Concentration: 0-400 μM
Incubation Time: 48 hours
Result: Showed antiproliferative activity with IC50s of 78.88, 96.83, 43.89, 58.55 μM for A2780, HeLa, K562, SiHa cells, respectively.

Apoptosis Analysis[1]

Cell Line: K562 cells
Concentration: 20 μM, 40 μM, 60 μM
Incubation Time: 48 hours
Result: Demonstrated a concentration-dependent increase in apoptosis of K562 cells, with apoptotic rates of 7.06 %, 6.00 %, and 81.52 % at 20, 40, and 60 μM, respectively.

Cell Cycle Analysis[1]

Cell Line: K562 cells
Concentration: 20 μM, 40 μM, 60 μM
Incubation Time: 48 hours
Result: The percentage of cells in the G0 / G1 phase was significantly increased from 30.58 % to 61.74 % with DNMT1-IN-3 at 60 μM.
Molecular Weight

487.72

Formula

C23H13Cl3N2O4
CAS No.
SMILES

O=C(O)[C@@H](N(C(C1=C2C=CC=C1)=O)C2=O)CN3C4=C(C5=C3C=CC(Cl)=C5)C=C(Cl)C=C4Cl
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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DNMT1-IN-3 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:

DNMT1-IN-33025012-68-1DNA MethyltransferaseDNMTsDNA MTasesA2780HeLaK562SiHaDNMT1 inhibitorCancerHematologic tumorInhibitorinhibitorinhibit

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