PAIR2 | IRE1α inhibitor | Probechem Biochemicals

Chemical Structure : PAIR2

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PAIR2 (IRE1α inhibitor PAIR2)

货号: PC-49054Not For Human Use, Lab Use Only.

PAIR2 is a partial antagonist of IRE1α RNase (PAIR) that fully engage IRE1α's kinase domain (Ki=8.8 nM) but only partially inhibits its RNase activity.

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生物&药学活性

PAIR2 is a partial antagonist of IRE1α RNase (PAIR) that fully engage IRE1α's kinase domain (Ki=8.8 nM) but only partially inhibits its RNase activity.
Unlike KIRAs, PAIR2 partially displaces helix-αC from an active conformation, and only reduce IRE1α's dimerization affinity.
PAIR2 demonstrated a similar ability to inhibit IRE1α's kinase activity as KIRA8 in vitro and in cells.
PAIR2 affect B-lymphocytes to differentiate into immunoglobulin-producing plasma cells.
PAIR2 is capable of completely occupying IRE1α's ATP-binding site in cells and can block the ability of a potent KIRA to inhibit XBP1 splicing.

物理化学性质&存储条件

分子量	590.598
分子式	C27H26F4N6O3S
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	(S)-2,2,2-trifluoro-N-(2-fluoro-3-methyl-4-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)ethane-1-sulfonamide

参考文献

1. Feldman HC, et al. Nat Chem Biol. 2021 Nov;17(11):1148-1156.

PAIR2 (IRE1α inhibitor PAIR2)

生物&药学活性

物理化学性质&存储条件

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PAIR2 (IRE1α inhibitor PAIR2)

生物&药学活性

物理化学性质&存储条件

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