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B I09

Catalog No.GC33406

B I09 Chemical Structure

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Sample solution is provided at 25 µL, 10mM.

Quality Control

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Protocol

Animal experiment:

Mice[2]Mice are intraperitoneally injected with B I09 (50 mg/kg) on the first 5 days of each week for 3 weeks[2].

References:

[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.

Background

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].

[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.

Chemical Properties

Cas No. 1607803-67-7 SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES OC1=CC=C(C2=C(CNCC2)C3=O)C(O3)=C1C4OCCCO4
Formula C16H17NO5 M.Wt 303.31
Solubility DMSO: 8.33 mg/mL (27.46 mM) Storage 4°C, protect from light
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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