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APY29

Catalog No.
B3288
IRE1α inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$165.00
In stock
Evaluation Sample
$28.00
In stock
10mg
$130.00
In stock
25mg
$275.00
In stock
50mg
$450.00
In stock

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Email: [email protected]

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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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt332.36
Cas No.1216665-49-4
FormulaC17H16N8
Solubility≥16mg/mL in DMSO
Chemical Name(E)-N-(6-((5-cyclopropyl-1H-pyrazol-3-yl)imino)-1,6-dihydropyrimidin-2-yl)-1H-benzo[d]imidazol-6-amine
SDFDownload SDF
Canonical SMILESC1(C2=CC(/N=C(N3)\C=CN=C3NC4=CC5=C(N=CN5)C=C4)=NN2)CC1
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Quality Control

Chemical structure

APY29