APY29

  • Catalog number
    2591-25
  • Price
    Please ask
  • Size
    25 mg
  • Alternative_name
    N2-1H-Benzimidazol-6-yl-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine
  • Description
    APY29 is a highly potent and selective allosteric modulator of IRE1α. Under endoplasmic reticulum (ER) stress, unfolded proteins accumulate in the ER to activate the ER transmembrane kinase/endoribonuclease (RNase)—IRE1α. IRE1α oligomerizes, autophosphorylates, and initiates splicing of XBP1 mRNA, thus triggering the unfolded protein response (UPR). APY29 Inhibits IRE1α autophosphorylation (IC₅₀ = 280 nM) and activates IRE1αRNase activity. As dysregulation of the UPR has been implicated in a variety of cell degenerative and neoplastic disorders, small molecule modulators of IRE1α should be very useful in understanding UPR’s role in pathophysiology and to develop drugs for ER stress-related diseases.
  • CAS Number
    1216665-49-4
  • Structure Available
    Y
  • Salt Form
    No
  • Molecular Formula
    C₁₇H₁₆N₈
  • Molecular Weight
    332.36
  • Cell Permeable
    yes
  • Purity
    ≥98% by HPLC
  • Solubilities
    DMSO (>30 mg/ml)
  • Handling
    Protect from light and air
  • Tag Line
    A highly potent and selective allosteric modulator of IRE1α
  • Storage Condition
    -20°C
  • Shipping Condition
    Gel pack
  • Shelf Life
    36 months
  • SMILES
    C1(NC2=CC(NC=N3)=C3C=C2)=NC=CC(NC4=NNC(C5CC5)=C4)=N1
  • InChi
    InChI=1S/C17H16N8/c1-2-10(1)13-8-16(25-24-13)22-15-5-6-18-17(23-15)21-11-3-4-12-14(7-11)20-9-19-12/h3-10H,1-2H2,(H,19,20)(H3,18,21,22,23,24,25)
  • InChi Key
    WJNBSTLIALIIEW-UHFFFAOYSA-N
  • MSDS Available
    Yes
  • Gene target
    APY29  
  • Short name
    APY29
  • Alternative name
    APY29
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