CPUY074020

SKU: orb1709985

Description

CPUY074020 is a potent, orally bioavailable small molecule inhibitor of the histone methyltransferase G9a, exhibiting an IC50 of 2.18 µM. It demonstrates anti-proliferative activity in cellular assays and serves as a valuable chemical probe for epigenetic research in oncology and other fields involving histone methylation.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 902279-44-1
• MW: 416.52
• Purity: 99.07% (May vary between batches)
• Formula: C₂₅H₂₈N₄O₂
• SMILES: N(CCN1CCCC1)C2=C3C=4C(C(=C2)N5CCCCC5)=NOC4C=6C(C3=O)=CC=CC6
• Target: Histone Methyltransferase
• Solubility: DMSO:4.17 mg/mL (10.01 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.4 mM)

Bioactivity

• Target IC50:
  G9a:2.18 μM
• In Vivo:
  CPUY074020 shows reasonable PK properties, with a T1/2 value of 4.0 hours and an oral bioavailability of 55.5% at an oral dose of 10 mg/kg.
• In Vitro:
  CPUY074020 (2.5-10μM ; 48 hours) dose-dependently de-regulates H3K9 trimethylation. CPUY074020 (2-8μM; 24 hours) induces cell death through apoptosis.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CPUY 074020, CPUY074020, CPUY-074020, HistoneMethyltransferase, Histone Methyltransferase, G9a

Compound Identifiers

PubChem CID

20867958