GSK046 - 10mM in DMSO, high purity , CAS No.2474876-09-8

Item Number

G422850

• Specifications & Purity: 10mM in DMSO
• Biochemical and Physiological Mechanisms: GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET (bromodomain and extraterminal domain) with IC50 of 264 nM, 98 nM, 49 nM and 214 nM for BRD2_BD2, BRD3_BD2, BRD4_BD2 and BRDT_BD2, respectively. GS
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads

Product Description

Information

GSK046 GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET (bromodomain and extraterminal domain) with IC50 of 264 nM, 98 nM, 49 nM and 214 nM for BRD2 BD2 , BRD3 BD2 , BRD4 BD2 and BRDT BD2 , respectively. GSK046 exhibits immunomodulatory activity.

Targets

BRD4_BD2 (Cell-free assay); BRD3_BD2 (Cell-free assay); BRDT_BD2 (Cell-free assay); BRD2_BD2 (Cell-free assay) 49 nM; 98 nM; 214 nM; 264 nM

In vitro

GSK046 shows an excellent level of selectivity for the BET family with no measurable activity for non-BET bromodomains. GSK046 is tested in an LPS-stimulated peripheral blood mononuclear cell (PBMC) cellular assay. After stimulation, these immune cells release a range of cytokines and chemokines, including monocyte chemoattractant protein 1 (MCP-1/CCL2). GSK046 also inhibits MCP-1 production (pIC50 = 7.5) with a minimal drop-off from the biochemical BRD4 BD2 potency observed.

In vivo

GSK046 has suitable physicochemical and pharmacokinetic properties to be utilized and it has also been demonstrated that a highly selective BD2 inhibitor retains the ability to potently inhibit MCP-1 cytokine release in a cellular and whole blood context. GSK046 proves useful for further biological profiling. GSK046 is efficacious in a broad range of inflammatory pathologies and selective BD2 inhibition may be a useful new therapeutic strategy for immunoinflammatory diseases.

Cell Research(from reference)

Cell lines：PBMCs, hepatocytes 

Concentrations：0.5 μM 

Incubation Time：5 min, 10 min, 20 min, 40 min, 60 min, 120 min