2. Cell Cycle/DNA Damage Apoptosis Protein Tyrosine Kinase/RTK
  3. IRE1 Apoptosis FGFR
  4. PAIR2

PAIR2 is a highly selective inhibitor targeting the kinase domain of human IRE1α, with a Ki value of 8.8 nM against human IRE1α. PAIR2 fully occupies the ATP-binding site of the IRE1α kinase domain, partially antagonizes the ribonuclease activity of IRE1α, specifically inhibits regulated IRE1α-dependent decay (RIDD) and its mediated substrate cleavage, while preserving the splicing function of Xbp1 mRNA. PAIR2 also promotes the differentiation of B cells into plasma cells, blocks IRE1α-induced cell apoptosis, and restores the expression of Fgfr2 mRNA in AT2 cells. PAIR2 effectively reaches a steady-state concentration in the lung tissues of Mus musculus, and serves as an important tool for investigating the function of the IRE1α signaling pathway in diseases such as pulmonary fibrosis.

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PAIR2

PAIR2 Chemical Structure

CAS No. : 2771006-54-1

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PAIR2 Related Antibodies

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Description

PAIR2 is a highly selective inhibitor targeting the kinase domain of human IRE1α, with a Ki value of 8.8 nM against human IRE1α. PAIR2 fully occupies the ATP-binding site of the IRE1α kinase domain, partially antagonizes the ribonuclease activity of IRE1α, specifically inhibits regulated IRE1α-dependent decay (RIDD) and its mediated substrate cleavage, while preserving the splicing function of Xbp1 mRNA. PAIR2 also promotes the differentiation of B cells into plasma cells, blocks IRE1α-induced cell apoptosis, and restores the expression of Fgfr2 mRNA in AT2 cells. PAIR2 effectively reaches a steady-state concentration in the lung tissues of Mus musculus, and serves as an important tool for investigating the function of the IRE1α signaling pathway in diseases such as pulmonary fibrosis[1][2].

IC50 & Target

IRE1α

8.8 nM (Ki)

FGFR2

 

In Vitro

PAIR2 (1-10 μM; 1 h + 6 h doxycycline (HY-N0565)) dose-dependently blocks doxycycline-induced autophosphorylation of IRE1α in INS-1::PCMV/2xTetO cells[1].
PAIR2 (0.5-10 μM; 1 h+2 h DTT (HY-15917)) maintains XBP1 mRNA splicing in parental INS-1 cells subjected to DTT stress[1].
PAIR2 (2 μM; 24 h Thapsigargin (HY-13433)) rescues Fgfr2 mRNA expression in serum-free, feeder-free primary mouse AT2 organoids under Thapsigargin stress, while preserving IRE1α-mediated Xbp1 splicing[2].
PAIR2 (2 μM; 3-d) fails to prevent the conversion of primary serum-free, feeder-free mouse AT2 cells to DATCs when pemigatinib directly blocks the Fgfr signaling pathway[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PAIR2 Related Antibodies

Western Blot Analysis[1]

Cell Line: INS-1::PCMV/2xTetO rat insulinoma cells (doxycycline-inducible IRE1α overexpression)
Concentration: 1, 3, 10 μM
Incubation Time: 1 h (PAIR2 pre-incubation); 6 h (doxycycline treatment)
Result: Dose-dependently blocked doxycycline-induced IRE1α autophosphorylation, reducing phosphorylated IRE1α levels to near baseline at concentrations ≥3 μM, with equivalent potency to KIRA8.

RT-PCR[1]

Cell Line: parent INS-1 rat insulinoma cells
Concentration: 0.5, 1, 3, 10 μM
Incubation Time: 1 h (PAIR2 pre-incubation); 2 h (DTT treatment)
Result: Preserved DTT-induced XBP1 mRNA splicing at all tested concentrations, with no significant reduction in splicing percentage relative to DTT-only treated cells (all P values > 0.05, non-significant).
In Vivo

Selective inhibition of RIDD with PAIR2 (30 mg/kg; i.p.; twice daily) reduces AT2 cell differentiation into profibrotic transitional cells and protects C57BL/6 mice from Bleomycin (HY-108345)-induced pulmonary fibrosis[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (10-20 week-old, both male and female, bleomycin-induced pulmonary fibrosis)[2]
Dosage: 30 mg/kg
Administration: i.p.; twice daily; starting 1 day before bleomycin exposure and continuing through study end
Result: Reduced fraction of trace+Krt8+ / trace+ cells compared to vehicle control at day 10 post-bleomycin exposure.
Significantly lowered lung hydroxyproline content and reduced fibrillar collagen deposition via picrosirius red staining at day 14 post-bleomycin exposure.
Derepressed expression of canonical RIDD target Bloc1s1 in lung tissue.
Did not significantly affect Xbp1 splicing.
Molecular Weight

590.59

Formula

C27H26F4N6O3S
CAS No.
SMILES

CC(C(F)=C(NS(CC(F)(F)F)(=O)=O)C1=C2C=CC=C1)=C2OC3=NC=CC=C3C4=NC(N[C@H]5CCCNC5)=NC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PAIR2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PAIR22771006-54-1PAIR 2PAIR-2IRE1ApoptosisFGFRInositol requiring enzyme 1Fibroblast growth factor receptorregulated IRE1α-dependent decaypulmonary fibrosisIRE1α kinase domainAT2 cellXbp1 mRNA splicingDATPsB cellimmunoglobulin-secreting plasma cellsFgfr2 mRNAIRE1α RNase activityInhibitorinhibitorinhibit

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