GSK2801

SKU: orb1223261

Description

GSK2801 is a A Selective Chemical Probe for BAZ2B/A bromodomains. BAZ2A/B belong to a family of ubiquitously expressed bromodomain containing proteins. Proteins of the BAZ family are characterized by a carboxy-terminal bromodomain adjacent to a PHD finger and a WACZ motif. In addition four other conserved motifs are typically found in the N-terminus of BAZ family members, namely the LH motif (a leucine-rich helical domain), the ZB2 motif and the BAZ 1 and BAZ 2 motifs. Little is known about the biological function of BAZ2B but it has been suggested to regulate nucleosome mobilization by the ATP-dependent chromatin remodeling factor ISWI.

Key Properties

• CAS Number: 1619994-68-1
• MW: 371.45
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₁NO₄S
• SMILES: CCCOc1cc2c(cc(n2cc1)C(=O)C)c1ccccc1S(=O)(=O)C
• Target: TAM Receptor
• Solubility: DMSO : 50 mg/mL. 134.61 mM; H2O : < 0.1 mg/mL

Bioactivity

• In Vivo:
  In order to determine the suitability of GSK2801 for In vivo experiments, pharmacokinetic parameters after intraperitoneal and oral dosing to male CD1 mice is measured. GSK2801 has reasonable In vivo exposure after oral dosing, modest clearance, and reasonable plasma stability.
• In Vitro:
  GSK2801 binds TAF1 L(2) with an affinity KB of 0.31 μM (KD: 3.2 μM) and a binding enthalpy change ΔH of 8.6 kcal/mol. ITC experiments using the bromodomain of BRD9 results in the determination of an affinity KB of 0.826 μM (KD: 1.1 μM) and ΔH of 9.8 kcal/mol. GSK2801 or RNAi knockdown of BAZ2A/B with JQ1 selectively displaced BRD2 at promoters/enhancers of ETS-regulated genes. In 2D cultures, enhances displacement of BRD2 from chromatin by combination drug treatment induced senescence. In spheroid cultures, combination treatment induces cleaved caspase-3 and cleaved PARP characteristic of apoptosis in tumor cells. Thus, GSK2801 blocks BRD2-driven transcription in combination with BET inhibitor and induces apoptosis of TNBC.

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

GSK2801 | GSK-2801 | GSK 2801

Quick Database Links

Gene Symbol

TAM Receptor