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Chemical Structure : PAIR2
Catalog No.: 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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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.
| M.Wt | 590.598 | |
| Formula | C27H26F4N6O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Feldman HC, et al. Nat Chem Biol. 2021 Nov;17(11):1148-1156.
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