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| Targets |
B-I09 targets IRE1α (inositol-requiring enzyme 1 alpha), a key sensor of the unfolded protein response (UPR). It is a cell-permeable IRE-1 RNase inhibitor with an IC50 of 1.23 µM. It blocks the IRE-1/XBP1 pathway. By inhibiting IRE1α RNase activity, it prevents XBP1 mRNA splicing and reduces ER stress signaling.
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| ln Vitro |
I09 has an IC50 of 1230 nM, making it an inhibitor of IRE-1 RNase[1]. Applying this inhibitor (B I09) to CLL cells causes symptoms similar to XBP-1 deficiency, such as increased IRE-1 expression and disrupted BCR signaling. B I09 has the ability to efficiently block the expression of XBP-1 in LPS-stimulated B cells and the splicing of XBP1 mRNA in human WaC3 cells [2].
In vitro, B-I09 inhibits IRE-1 RNase activity with an IC50 of 1.23 µM (1230 nM). It inhibits XBP1 mRNA splicing in human WaC3 cells and LPS-stimulated B cells. It exhibits an inhibitory effect on the growth of human chronic lymphocytic leukemia (CLL) cells in vitro. |
| ln Vivo |
I09 has a half-life of roughly 1.5 hours, and 15 minutes after treatment, mouse plasma reaches peak concentrations of about 39 μM. B I09 administration to mice with CLL tumors prevents the spread of leukemia by triggering apoptosis without harming the body as a whole [2].
In vivo, B-I09 promotes CLL regression in a mouse model. It can be used to study CLL cells and simulate XBP-1 deficiency. It reduces ER stress signaling and modulates cell survival and inflammation. Detailed in vivo efficacy data including tumor regression are available in preclinical literature. |
| Enzyme Assay |
In vitro enzyme assays for B-I09 typically involve measuring the inhibition of IRE1α RNase activity. The enzyme is incubated with a substrate (e.g., XBP1 mRNA or a fluorescent RNA probe) and varying concentrations of the compound. RNase activity is measured by monitoring substrate cleavage. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cell-based assays for B-I09 involve culturing CLL cells or other cell lines in appropriate media. Cells are treated with B-I09 at concentrations ranging from 0.1 µM to 10 µM for 24-72 hours. XBP1 mRNA splicing is measured by RT-PCR. Cell viability is assessed by MTT or CellTiter-Glo assays. ER stress markers are measured by Western blot or qPCR. Apoptosis is evaluated by flow cytometry.
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| Animal Protocol |
In vivo animal experiments for B-I09 typically involve administration to tumor-bearing mice (CLL models) via oral gavage or intraperitoneal injection. Tumor growth or regression is monitored. XBP1 splicing and ER stress markers are assessed in tumor tissues. Pharmacokinetic parameters are evaluated by measuring compound levels in blood and tissues. Toxicity is assessed by monitoring body weight and organ histology.
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| ADME/Pharmacokinetics |
B-I09 (molecular weight ~350-400) is cell-permeable. It is soluble in DMSO (8.33 mg/mL). Detailed pharmacokinetic parameters including absorption, distribution, metabolism, and excretion are available in preclinical literature. It has suitable properties for in vivo studies in mouse models.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for B-I09 from the search results. As an IRE1α inhibitor, potential toxicity may include effects on ER stress responses in normal tissues. Comprehensive toxicological evaluation including acute, subchronic, and genotoxicity studies has likely been conducted. Standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
B-I09 (CAS#: 1607803-67-7) is a cell-permeable IRE1α RNase inhibitor (IC50 = 1.23 µM). It inhibits XBP1 mRNA splicing and reduces ER stress signaling. It inhibits CLL cell growth and promotes CLL regression in mouse models. It is a research tool for studying the UPR and ER stress.
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| Molecular Formula |
C16H17NO5
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|---|---|
| Molecular Weight |
303.309884786606
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| Exact Mass |
303.11
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| CAS # |
1607803-67-7
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| PubChem CID |
86290458
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| Appearance |
Yellow to brown solid powder
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| LogP |
0.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
22
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| Complexity |
485
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1NCCC2C3=CC=C(O)C(C4OCCCO4)=C3OC(=O)C1=2
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| InChi Key |
UYYMWNUDIOPESF-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
7-(1,3-dioxan-2-yl)-8-hydroxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~8.33 mg/mL (~27.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.24 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2970 mL | 16.4848 mL | 32.9696 mL | |
| 5 mM | 0.6594 mL | 3.2970 mL | 6.5939 mL | |
| 10 mM | 0.3297 mL | 1.6485 mL | 3.2970 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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