1. Epigenetics
  2. DNA Methyltransferase
  3. DY-46-2

DY-46-2 

Cat. No.: HY-151136
Handling Instructions

DY-46-2 is a high potency and selectivity novel non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor with an IC50 value of 0.39 μM.

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

DY-46-2 Chemical Structure

DY-46-2 Chemical Structure

CAS No. : 1105110-83-5

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Description

DY-46-2 is a high potency and selectivity novel non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor with an IC50 value of 0.39 μM[1].

IC50 & Target

DNMT3A

0.39 μM (IC50)

In Vitro

DY-46-2 (0.1-100 μM, 24, 48 and 72 h) has an inhibitory activity of DNMT3A with an IC50 value of 0.39 μM, which increases linearly with DNA concentration (IDT-01)[1].
DY-46-2 (0.1-100 μM, 24, 48 and 72 h) has inhibitory activity against DNMT1, DNMT3B and G9a with IC50 values of 13.0 μM, 105 μM and >500 μM, respectively[1].
DY-46-2 (0.1-100 μM, 24, 48 and 72 h) has cell viability in cancer cells with IC50 values of 0.7 μM, 0.3 μM, 0.7 μM, 0.5 μM, 2.1 μM, 1.7 μM and 91 μM for THP-1, HCT116, U937, K562, A549, DU145 and PBMC cell, respectively[1].
DY-46-2 (0.1-100 μM, 24, 48 and 72 h) markedly inhibits the proliferation of cancer cells and shows low cytotoxicity in peripheral blood mononuclear cells (PBMCs)[1].
DY-46-2 (1 μM, 72 h) obviously decreases DNMT3A protein levels, as well as reactive expression of a silenced TSG (p53) in HCT116 cells[1].

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

Cell Viability Assay[1]

Cell Line: THP-1, HCT116, U937, K562, A549, DU145 and PBMC cell
Concentration: 0.1-100 μM
Incubation Time: 24, 48 and 72 h
Result: Had remarkable inhibitory potency in the dose- and time-dependent manners and no cytotoxicity in non-tumoral PBMCs (IC50 >100 μM).

Cell Proliferation Assay[1]

Cell Line: THP-1, HCT116, U937, K562, A549, DU145 and PBMC cell
Concentration: 0.1-100 μM
Incubation Time: 24, 48 and 72 h
Result: Exhibited high anti-proliferative activity with a micromolar range cytotoxicity in all cancer cells.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 1 μM
Incubation Time: 72 h
Result: Decreased DNMT3A and p53 protein levels in the HCT116 cells, apparently sufficient to reactive expression of a silenced TSG (p53).
Molecular Weight

446.48

Formula

C19H22N6O5S

CAS No.
SMILES

O=C(C1=C(C)OC(N=CN2CCN3CCCC3)=C1C2=O)NC4=CC=C(S(=O)(N)=O)N=C4

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
References
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DY-46-2
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