UNC0642

SKU: orb1303097

Description

UNC0642 is a potent and selective small-molecule inhibitor of the histone methyltransferases G9a and GLP, exhibiting IC50 values below 2.5 nM. It is widely used in epigenetic research to probe histone H3K9 methylation in both cellular and animal models, facilitating studies in oncology, neurobiology, and developmental biology.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1481677-78-4
• MW: 546.7
• Purity: 99.50% (May vary between batches)
• Formula: C₂₉H₄₄F₂N₆O₂
• SMILES: COc1cc2c(NC3CCN(CC3)C(C)C)nc(nc2cc1OCCCN1CCCC1)N1CCC(F)(F)CC1
• Target: Histone Methyltransferase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.66 mM);DMSO:50 mg/mL (91.46 mM)

Bioactivity

• Target IC50:
  GLP:<2.5 nM|G9a:<2.5 nM
• In Vivo:
  UNC0642 (5 mg/kg, i.p.) results in a plasma Cmax of 947 ng/mL and an AUC of 1265 h·ng/ml.
• In Vitro:
  UNC0642 (Ki: 3.7±1 nM) is competitive with the peptide substrate and non-competitive with the cofactor SAM. UNC0642 is more than 300-fold selective for G9a and GLP over a broad range of kinases, transporters, GPCRs, and ion channels. UNC0642 exhibits high potency at low cell toxicity, reducing the H3K9me2 mark, and good separation of functional potency in a number of cell lines.
• Cell Research:
  MDA-MB-231, PC3, and U2OS cells are treated with UNC0642 for 48 h. Cell viability assays are performed by incubating cells with 0.1 mg/mL of resazurin for 3 – 4 h. Resazurin reduction is monitored with 544 nm excitation, measuring fluorescence at 590 nm.
• Animal Research:
  Mouse: Standard PK studies are performed using male Swiss albino mice. Plasma and brain concentrations are measured at 0.08, 0.25, 0.5, 1, 2, 4, 8, and 24 h following UNC0642 (5 mg/kg, i.p.). The compound concentration at each time point in plasma or brain is the average value from 3 test animals.

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

Histone Methyltransferase, HistoneMethyltransferase, G9a/GLP, Inhibitor, inhibit, UNC 0642, UNC0642, UNC-0642

Compound Identifiers

PubChem CID

53315878