包装: | 1mg |
市场价: | 1197元 |
Cell lines | Jurkat cells; Human pulmonary artery endothelial cells (HPAECs) |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 20 μM, 16-18h |
Applications | In Jurkat cells, GI 254023X inhibited cell proliferation and increased apoptosis in a concentration-dependent manner. Compared with control group, GI 254023X up-regulated the expression of Notch1 while down-regulated the expression of cleaved Notch1 in a time-dependent way. GI254023X also reduced the levels of MCL-1 and Hes-1 mRNA transcripts. In human pulmonary artery endothelial cells (HPAECs), GI254023X inhibited VE-cadherin cleavage and completely protected HPAECs from Hla-mediated barrier disruption. |
Animal models | BALB/c mice injected with endotoxin-free recombinant Hla |
Dosage form | 200 mg/kg/day, dilution in 0.1 M carbonate buffer, 3-day period, intraperitoneal injection |
Application | In BALB/c mice injected with endotoxin-free recombinant Hla, GI254023X enhanced vascular integrity, manifest by limited dye extravasation, suggested that GI254023X may afford protection against lethal infection. Mice were treated with either DMSO or GI254023X then infected with 5×107 CFUs S. aureus Newman. GI254023X-treated mice were less ill in appearance and demonstrated prolongation of time to death. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
产品描述 | Description:IC50: 5.3 nM (ADAM10) |