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PAIR1

Chemical Structure : PAIR1

CAS No.: 2771006-58-5

PAIR1 (IRE1α inhibitor PAIR1)

Catalog No.: PC-49055Not For Human Use, Lab Use Only.

PAIR1 is a partial antagonist of IRE1α RNase (PAIR) that fully engage IRE1α's kinase domain (Ki=220 nM) but only partially inhibit its RNase activity.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PAIR1 is a partial antagonist of IRE1α RNase (PAIR) that fully engage IRE1α's kinase domain (Ki=220 nM) but only partially inhibit its RNase activity.
Unlike KIRAs, PAIR1 partially displaces helix-αC from an active conformation, and only reduce IRE1α's dimerization affinity.
PAIR1 spares XBP1 splicing but blocks Regulated IRE1α Dependent Degradation (RIDD) outputs in cells.
PAIR1 largely preserved XBP1 mRNA splicing and expression of the frame-shifted Xbp1s transcription factor protein in cellular systems.
PAIR1 inhibits IRE1α-dependent mRNA decay and apoptosis in INS-1 cells that conditionally overexpress IRE1α.
PAIR1 affect B-lymphocytes to differentiate into immunoglobulin-producing plasma cells.

Physicochemical Properties

M.Wt 558.580
Formula C26H25F3N6O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-2,2,2-trifluoro-N-(4-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)ethane-1-sulfonamide

References

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

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