IRE1α kinase-IN-1

CAS No. 2328097-41-0

IRE1α kinase-IN-1 ( —— )

Catalog No. M28763 CAS No. 2328097-41-0

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 335 Get Quote
10MG 500 Get Quote
25MG 806 Get Quote
50MG 1098 Get Quote
100MG 1485 Get Quote
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Biological Information

  • Product Name
    IRE1α kinase-IN-1
  • Note
    Research use only, not for human use.
  • Brief Description
    IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform.
  • Description
    IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM).(In Vitro):IRE1α kinase-IN-1 (compound 31) prevents endoplasmic reticulum stress-induced IRE1α oligomerization and phosphorylation, and inhibits endoribonuclease activity in human cells.IRE1α kinase-IN-1 and is very high selectivity with >70% inhibition of only 4/455 kinases. IRE1α kinase-IN-1 inhibits recombinant G547 IRE1α KEN domain pS274 autophosphorylation with an IC50 of 160 nM. IRE1α kinase-IN-1 inhibits tunicamycin-induced GFP-IRE1α foci in HEK293 cells with an IC50 of 0.74 μM. IRE1α kinase-IN-1 Inhibits ATP-site LanthaScreen tracer binding to recombinant dephosphorylated G547 IRE1α KEN with an IC50 of 0.27 μM.IRE1α kinase-IN-1 inhibits both tunicamycin- and thapsigargin-induced IRE1α-dependent splicing of XBP1 luciferase fusion mRNA in HEK293 cells with IC50s ranging 0.68-1.63 μM.IRE1α kinase-IN-1 (0-20 μM) inhibits IRE1α-dependent XBP1s mRNA expression in H929 cells.IRE1α kinase-IN-1 (0-20 μM) dose-dependently inhibits tunicamycin-induced expression of XBP1s in NCI-H929 cells.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Antibacterial
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2328097-41-0
  • Formula Weight
    505.0
  • Molecular Formula
    C26H26ClFN8
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    CN1CCC(CNc2cc(Cl)nn3c2ncc3-c(cc2nc(Nc3ccccc3)[nH]c2c2)c2F)CC1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Lo Re V 3rd, et al. Oral Azole Antifungal Medications and Risk of Acute Liver Injury, Overall and by Chronic Liver Disease Status. Am J Med. 2016 Mar;129(3):283-91.e5.
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