GSK1324726A (I-BET726) - 10mM in DMSO, high purity , CAS No.1300031-52-0

Item Number

G421169

• Specifications & Purity: 10mM in DMSO
• Biochemical and Physiological Mechanisms: GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads

Product Description

Information

GSK1324726A (I-BET726) GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively.

Targets

BRD4 (Cell-free assay); BRD3 (Cell-free assay); BRD2 (Cell-free assay) 22 nM; 31 nM; 41 nM

In vitro

In neuroblastoma cell lines, GSK1324726A inhibits cell growth and induces cytotoxicity. GSK1324726A also modulates expression of genes involved in apoptosis, signaling, and MYC-family pathways, including the direct suppression of BCL2 and MYCN.

In vivo

In the mouse SK–N-AS and CHP-212 models, GSK1324726A (15 mg/kg p.o.) results in tumor growth inhibition and down-regulation MYCN and BCL2 expression. In a mouse septic shock model, GSK1324726A (10 mg/kg i.v.) shows potent anti-inflammatory effects, and prevents death of diseased animals.

Cell Research(from reference)

Cell lines：LA-N-1, Kelly, LA1-55n, BE(2)-M17, BE(2)-C, KanTS, IMR32, LA-N-2, SK-N-SH, SK-N-BE(2), CHP-134, SK-N-AS, SH-SY5Y, SK-N-FI, CHP-212, LA1-5s, SK-N-DZ cells 

Concentrations：~10 μM 

Incubation Time：6 days