Molecular Formula | C25H23ClN2O3 |
Molar Mass | 434.91 |
Density | 1.304±0.06 g/cm3(Predicted) |
Boling Point | 707.3±60.0 °C(Predicted) |
Solubility | DMSO : ≥ 46 mg/mL (105.77 mM) |
pKa | 4.20±0.10(Predicted) |
Storage Condition | -20℃ |
Use | GSK1324726A is a potent selective BET protein inhibitor with high affinity binding to BRD2 (IC50=41 nM),BRD3 (IC50=31 nM) and BRD4 (IC50=22 nM). |
Target | BRD2; BRD3; BRD4 |
In vitro study | 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 study | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.299 ml | 11.497 ml | 22.993 ml |
5 mM | 0.46 ml | 2.299 ml | 4.599 ml |
10 mM | 0.23 ml | 1.15 ml | 2.299 ml |
5 mM | 0.046 ml | 0.23 ml | 0.46 ml |
biological activity | GSK1324726A(I-BET726) is a highly selective inhibitor of BET family proteins. the IC50 for BRD2, BRD3, and BRD4 is 41 nM, 31 nM, and 22 nM respectively. |
in vitro studies | 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 research | 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. |