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APY29

Catalog No.
B3288
IRE1α inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$149.00
In stock
Evaluation Sample
$30.00
In stock
10mg
$143.00
In stock
25mg
$303.00
In stock
50mg
$495.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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
Solubilityinsoluble in H2O; insoluble in EtOH; ≥16 mg/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 ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Chemical structure

APY29