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
200MG Get Quote Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

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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