1. Epigenetics
  2. Histone Methyltransferase
  3. CPUY074020

CPUY074020 

Cat. No.: HY-100757
Handling Instructions

CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity.

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

CPUY074020 Chemical Structure

CPUY074020 Chemical Structure

CAS No. : 902279-44-1

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Description

CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity[1].

IC50 & Target

IC50: 2.18 μM (G9a)[1]

In Vitro

CPUY074020 (2-8μM; 24 hours) induces cell death through apoptosis[1].
CPUY074020 (2.5-10μM ; 48 hours) dose-dependently de-regulates H3K9 trimethylation[1].

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 2 μM, 4 μM, 8 μM
Incubation Time: 24 hours
Result: Induced MCF-7 cells apoptosis.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 48 hours
Result: Dose-dependently de-regulated H3K9 trimethylation.
In Vivo

CPUY074020 exhibits reasonable PK properties, with an oral bioavailability of 55.5% and a T1/2 value of 4.0 hours at an oral dose of 10 mg/kg[1].

Animal Model: Mice
Dosage: 10 mg/kg
Administration: Oral administration
Result: t1/2=4.0 hours
Molecular Weight

416.52

Formula

C₂₅H₂₈N₄O₂

CAS No.

902279-44-1

SMILES

O=C1C2=CC=CC=C2C3=C4C1=C(NCCN5CCCC5)C=C(N6CCCCC6)C4=NO3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

CPUY074020CPUY 074020CPUY-074020Histone MethyltransferaseProteinlysinemethyltransferaseG9aInhibitorinhibitorinhibit

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