GSK6853

SKU: orb1304337

Description

GSK6853

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1910124-24-1
• MW: 409.48
• Purity: 99.08%
• Formula: C₂₂H₂₇N₅O₃
• SMILES: COc1ccccc1C(=O)Nc1cc2n(C)c(=O)n(C)c2cc1N1CCNC[C@H]1C
• Target: Epigenetic Reader Domain
• Solubility: DMSO:55 mg/mL (134.32 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.88 mM);Ethanol:81 mg/mL (197.81 mM)

Bioactivity

• Target IC50:
  BRPF1:8.1( IC50
• 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 tha the IP route of administration would be suitable for dosing this molecule in potential PKPD model.
• 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 minimiz the chance of off-target effects the recommended concentration is no higher than 1 μM in cell-based assay.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• 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