BRPF1-IN-3

SKU: orb1223706

Description

BRPF1-IN-3 is a potent, selective, membrane permeable BRPF1 bromodomain inhibitor with pIC50 of 7.1; shows 100- and >1000-fold selectivity over BRPF2 and BRPF3, respectively; exhibits an IC50 of 0.98 uM in cellular protein interaction assay (displacement of NanoLuc-tagged BRPF1 bromodomain from Halo-tagged histone H3.3).

Key Properties

• CAS Number: 901245-65-6
• MW: 394.475
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₆N₄O₃
• SMILES: O=C(NC1=C(N2CCCCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC
• Target: Bromodomain
• Solubility: DMSO: 10 mM （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vitro:
  GSK-5959 (3a) also displays selectivity over the closely related family members, BRPF2 (100-fold) and BRPF3 (>1000-fold). GSK-5959 (3a) exhibits an EC50 = 0.98 μM) in cellular NanoBRET assay. GSK-5959 has no effect on TRIM24 SUMOylation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK-5959 | GSK 5959 | GSK5959.

Quick Database Links

Gene Symbol

Bromodomain