Chemical Structure : IA107
CAS No.:
IA107
(IA-107)
Catalog No.: PC-25597Not For Human Use, Lab Use Only.
IA107 is a potent and selective inositol-requiring enzyme 1 alpha (IRE1α) inhibitor, inhibitsIRE1α and phosphorylated IRE1α RNase activity in FRET assay with IC50 of 16 nM and 9 nM, respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
IA107 is a potent and selective inositol-requiring enzyme 1 alpha (IRE1α) inhibitor, inhibitsIRE1α and phosphorylated IRE1α RNase activity in FRET assay with IC50 of 16 nM and 9 nM, respectively.
IA107 binds to IRE1α with ITC KD of 0.94 uM and MST KD of 1.36 uM.
IA107 shows binding affinity against p-IRE1α with MST KD of 152 nM.
IA107 prefers to bind to the dimeric form of IRE1α to inhibit its RNase activity.
IA107 shows minimal (<10%) to low (<30%) inhibitory activity at 5 uM in a kinase profiling assay, IA107 inhibits the kinase domain of the IRE1β (ERN2) isoform with an IC50 of 1440 nM in the LanthaScreenTM Eu kinase binding assay.
IA107 (5-50 uM) inhibited ER stress induced by tunicamycin and induced XBP1 mRNA splicing in A549 cells.
Physicochemical Properties
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M.Wt
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386.25
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Formula
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C19H16BrNO3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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3-(1-benzoyl-5-bromo-2-methyl-1H-indol-3-yl)propanoic acid
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References
1. Liu Y, et al. Nat Commun. 2025 Sep 26;16(1):8531.
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