| CAS |
No.1607803-67-7 |
| 英文名称 |
B I09 |
| 分子式 |
C16H17NO5 |
| 分子量 |
303.31 |
| 溶解性 |
Soluble in DMSO ≥1mg/mL(该产品在溶液状态不稳定，建议您现用现配，即刻使用。) |
| 纯度 |
≥98% |
| 外观(性状) |
Light yellow to brown Solid |
| 储存条件 |
Powder:2-8℃，2 years. |
| 靶点 |
IRE1 |
| 通路 |
ER Stress |
| 背景说明 |
B I09 是 IRE-1 核糖核酸酶的一个抑制剂。 |
| 生物活性 |
B I09 is an IRE-1 RNase inhibitor， with an IC50 of 1230 nM.[1-2] |
| IC50 |
IC50: 1230 nM (IRE-1 RNase)[1]. |
| In Vitro |
B I09 is an IRE-1 RNase inhibitor， with an IC50 of 1230 nM[1]. Treatment of CLL cells with this inhibitor (B I09) mimick XBP-1 deficiency， including upregulation of IRE-1 expression and compromised BCR signaling. B I09 is highly effective in inhibiting splicing of XBP1 mRNA in human WaC3 cells and the expression of XBP-1s in LPS stimulated B cells[2]. |
| In Vivo |
B I09 has a halflife of approximately 1.5 hours and reaches its peak concentration of approximately 39 μM in mouse plasma serum 15 minutes after administration. Administration of B I09 to CLL tumor-bearing mice suppress leukemic progression by inducing apoptosis and do not cause systemic toxicity[2]. |
| 动物实验 |
Mice[2]Mice are intraperitoneally injected with B I09 (50 mg/kg) on the first 5 days of each week for 3 weeks[2]. |
| 数据来源文献 |
[1]. Ranatunga S， et al. Synthesis of novel tricyclic chromenone-based inhibitors of IRE-1 RNase activity. J Med Chem. 2014 May 22;57(10):4289-301.
[2]. Tang CH， et al. Inhibition of ER stress-associated IRE-1/XBP-1 pathway reduces leukemic cell survival. J Clin Invest. 2014 Jun;124(6):2585-98. |
| 规格 |
1mg 5mg 10mg 50mg |
| 单位 |
瓶 |
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