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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-IRE1-IA107
IA107

Chemical Structure : IA107

CAS No.:

IA107 (IA-107)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 386.25
分子式 C19H16BrNO3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(1-benzoyl-5-bromo-2-methyl-1H-indol-3-yl)propanoic acid

参考文献

1. Liu Y, et al. Nat Commun. 2025 Sep 26;16(1):8531.

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