UNC0224

SKU: orb1307633

Description

UNC0224 is a potent and selective small molecule inhibitor of the histone methyltransferases G9a (Ki = 2.6 nM) and GLP. It is a valuable chemical probe for epigenetic research, enabling the study of histone methylation roles in cancer biology, neurodevelopment, and other cellular processes in both in vitro and in vivo models.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1197196-48-7
• MW: 485.67
• Purity: 99.80% (May vary between batches)
• Formula: C₂₆H₄₃N₇O₂
• SMILES: COc1cc2c(NC3CCN(C)CC3)nc(nc2cc1OCCCN(C)C)N1CCCN(C)CC1
• Target: Histone Methyltransferase
• Solubility: DMSO:35.71 mg/mL (73.53 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.06 mM)

Bioactivity

• Target IC50:
  G9a:15 nM|G9a:2.6 nM （ki）|G9a:23 nM （kd）|GLP:20-58 nM
• In Vitro:
  In G9a ECSD and CLOT assays, the IC50 values are 43 nM and 57 nM for UNC0224, respectively. In GLP ECSD and CLOT assays, the IC50 values are 50 nM and 58 nM for UNC0224, respectively. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3, and JMJD2E. In ITC experiments, the Kd of UNC0224 to the G9a protein is 23 nM.

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

chromatin, Inhibitor, Histone Methyltransferase, HistoneMethyltransferase, GLP, H3K9, G9a, p53, lysine, inhibit, K373, stabilized, SAR, PKMT, quinazoline, UNC0224, UNC-0224, UNC 0224

Compound Identifiers

PubChem CID

44251522