Home>>Signaling Pathways>> DNA Damage/DNA Repair>> IRE1>>APY29
APY29 Catalog No.GC17139

IRE1α inhibitor

Size Price Stock Qty
10mM (in 1mL DMSO)
$127.00
In stock
10mg
$97.00
In stock
25mg
$209.00
In stock
50mg
$333.00
In stock

Customer Review

Based on customer reviews.

Tel: (626) 353-8530 Email: sales@glpbio.com

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

View current batch:

Chemical Properties

Cas No. 1216665-49-4 SDF
Chemical Name (E)-N-(6-((5-cyclopropyl-1H-pyrazol-3-yl)imino)-1,6-dihydropyrimidin-2-yl)-1H-benzo[d]imidazol-6-amine
Canonical SMILES C1(C2=CC(/N=C(N3)\C=CN=C3NC4=CC5=C(N=CN5)C=C4)=NN2)CC1
Formula C17H16N8 M.Wt 332.36
Solubility ≥ 16mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

Background

APY29 is an inhibitor of IRE1α with IC50 value of 0.28μM [1].

IRE1α is a transmembrane protein in ER. It can be activated when unfolded proteins accumulate in ER. APY29 is found to interact with the ATP-binding site of wild-type IRE1α and activate the kinase activity of IRE1α even without upstream ER stress. APY29 acts as a slight activator and stabilizes IRE1α’s kinase domain in an alternative conformation. It is found to restore the ability of dephosphorylated IRE1α to cleave the substrate XBP1 up to about 60% of the levels of normal IRE1α. Furthermore, APY29 increases the oligomer/monomer ratio of IRE1α and finally displays a decrease of IRE1α trans-autophosphorylation [1].

References:
[1] Wang L, Perera BG, Hari SB, Bhhatarai B, Backes BJ, Seeliger MA, Schürer SC, Oakes SA, Papa FR, Maly DJ. Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors. Nat Chem Biol. 2012 Dec;8(12):982-9.