GSK6853

SKU: orb1304337

Description

GSK6853 is a highly selective, cell-permeable small molecule inhibitor targeting the BRPF1 bromodomain. It is a valuable chemical probe for epigenetic research, enabling the study of BRPF1 function in chromatin remodeling and gene regulation in both cellular and in vivo models.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1910124-24-1
• MW: 409.5
• Purity: >98%
• Formula: C₂₂H₂₇N₅O₃
• SMILES: COc1ccccc1C(=O)Nc1cc2n(C)c(=O)n(C)c2cc1N1CCNC[C@H]1C
• Target: Bromodomain
• Solubility: Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (25 mg/ml)

Bioactivity

• Target IC50:
  BRPF1:8.1(pIC50)
• In Vivo:
  In male CD1 mouse, following IV administration (1 mg/kg), GSK6853 demonstrates a high blood clearance of 107 mL/min/kg, a moderate volume of distribution (5.5 L/kg) and a moderate terminal half-life of 1.7 h. Oral administration (PO, 3 mg/kg) achieves a moderate systemic exposure, with a Cmax of 42 ng/mL and Tmax of 1.5 h, resulting in a bioavailability of 22%. The intraperitoneal route of administration (IP, 3 mg/kg) reaches a Cmax of 469 ng/mL and Tmax of 0.25 h, resulting in a bioavailability of 85%. The results indicate that the IP route of administration would be suitable for dosing this molecule in potential PKPD models.
• In Vitro:
  Screening GSK6853 against a panel of 48 unrelated assays reveals only off-target activities that are relatively weak compared to the BRPF1 potency. However, to minimize the chance of off-target effects , the recommended concentration is no higher than 1 μM in cell-based assays.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BRPF3, BRPF1, BRPF2, Inhibitor, inhibit, Epigenetic Reader Domain, EpigeneticReaderDomain, GSK6853, GSK-6853, GSK 6853

Compound Identifiers

PubChem CID

121232405