GSK1379725A

SKU: orb1308254

Description

GSK1379725A is a potent and selective small molecule ligand for the bromodomain of BPTF, exhibiting a binding affinity (Kd) of 2.8 µM. This compound serves as a valuable chemical probe for investigating the role of BPTF in chromatin remodeling and gene regulation, applicable in both in vitro biochemical and cellular studies.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1802251-00-8
• MW: 450.47
• Purity: 99.51%
• Formula: C₂₃H₂₃FN₆O₃
• SMILES: COC(=O)c1cccc(NC(=O)NC2CCN(C2)c2ccnc(Nc3ccc(F)cc3)n2)c1
• Target: Epigenetic Reader Domain
• Solubility: DMSO:50 mg/mL (111 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.44 mM)

Bioactivity

• Target IC50:
  BPTF:2.8 μM(Kd)
• In Vitro:
  GSK1379725A has proven to be selective towards Brd4, though comprehensive evaluation against other bromodomains is necessary. Searches in the ChEMBL database reveal its activity in only five cellular assays, indicating a potency (EC50) of 500 nM, with no kinase activity noted despite extensive screenings, especially with the PKIS library. NMR titration data showed a separation of 171 Hz between bound and unbound resonances of GSK1379725A, suggesting a maximum chemical exchange rate. Based on an assumed high association rate (e.g., similar to chymotrypsin: proflavin at 1.2×108 M-1 s-1), the dissociation constant (Kd) is approximately 8 μM. For more precise Kd measurement, ITC was employed with unlabeled BPTF, yielding a Kd of 2.8 μM, aligning with the observed intermediate exchange resonance broadening detected by PrOF NMR, thus confirming the specificity and binding characteristics of GSK1379725A.

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

inhibit, Inhibitor, Epigenetic Reader Domain, EpigeneticReaderDomain, GSK1379725A, GSK-1379725A, BPTF

Compound Identifiers

PubChem CID

44525934