For research use only. Not for therapeutic Use.
B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
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].
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].
| Catalog Number | I011362 |
| CAS Number | 1607803-67-7 |
| Synonyms | 7-(1,3-dioxan-2-yl)-8-hydroxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one |
| Molecular Formula | C16H17NO5 |
| Purity | ≥95% |
| InChI | InChI=1S/C16H17NO5/c18-12-3-2-10-9-4-5-17-8-11(9)15(19)22-14(10)13(12)16-20-6-1-7-21-16/h2-3,16-18H,1,4-8H2 |
| InChIKey | UYYMWNUDIOPESF-UHFFFAOYSA-N |
| SMILES | C1COC(OC1)C2=C(C=CC3=C2OC(=O)C4=C3CCNC4)O |
| Reference | [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. |
