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Cat. No.: HY-161694

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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 K_D 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.

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

CAS No.: 3025012-68-1
Formula: C₂₃H₁₃Cl₃N₂O₄
Molecular Weight:487.72

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (279 KB)

DNMT1-IN-3 Chemical Structure

CAS No.: 3025012-68-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

DNMT1

0.777 μM (IC₅₀)

All DNA Methyltransferase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	78.88 μM Compound: (S)-7t-2	Antiproliferative activity against human A2780 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human A2780 cells incubated for 48 hrs by MTT assay	[PMID: 38823264]
HeLa	IC₅₀	96.83 μM Compound: (S)-7t-2	Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay	[PMID: 38823264]
K562	IC₅₀	43.89 μM Compound: (S)-7t-2	Antiproliferative activity against human K562 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human K562 cells incubated for 48 hrs by MTT assay	[PMID: 38823264]
SiHa	IC₅₀	58.55 μM Compound: (S)-7t-2	Antiproliferative activity against human SiHa cells incubated for 48 hrs by MTT assay Antiproliferative activity against human SiHa cells incubated for 48 hrs by MTT assay	[PMID: 38823264]

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.

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.

Chemical Information

CAS No. 3025012-68-1
Molecular Weight 487.72
Formula C₂₃H₁₃Cl₃N₂O₄
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Liu J, et al. Identification of 3-(9H-carbazol-9-yl)-2-(1,3-dioxoisoindolin-2-yl)propanoic acids as promising DNMT1 inhibitors. Eur J Med Chem. Published online May 27, 2024. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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