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Biochem/physiol Actions
Cell penetrant, potent and selective ATP-competitive partial antagonist of the IRE1α RNase activity, while affording quantitative kinase activity inhibition
PAIR1 is a cell penetrant, potent and selective ATP-competitive partial antagonist of the IRE1α (endoplasmic reticulum to nucleus signaling 1) RNase activity, while affording quantitative kinase activity inhibition. PAIR1 partially antagonize the IRE1α RNase at full occupancy of the kinase. In β-cells PAIR1 allows adaptive splicing of Xbp1 mRNA while suppressing destructive ER mRNA endonucleolytic decay and apoptosis.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | O=S(NC(C=C1)=C2C(C=CC=C2)=C1OC3=NC=CC=C3C4=CC=NC(N[C@@H]5CNCCC5)=N4)(CC(F)(F)F)=O |
| InChI | 1S/C26H25F3N6O3S/c27-26(28,29)16-39(36,37)35-22-9-10-23(19-7-2-1-6-18(19)22)38-24-20(8-4-13-31-24)21-11-14-32-25(34-21)33-17-5-3-12-30-15-17/h1-2,4,6-11,13-14,17,30,35H,3,5,12,15-16H2,(H,32,33,34)/t17-/m0/s1 |
| InChI key | LVBYPSVRFGNRPW-KRWDZBQOSA-N |
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