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APY29

Catalog No.GC17139

IRE1α inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

APY29 Chemical Structure

Cas No.: 1216665-49-4

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

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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

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 Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.0088 mL 15.0439 mL 30.0879 mL
5 mM 0.6018 mL 3.0088 mL 6.0176 mL
10 mM 0.3009 mL 1.5044 mL 3.0088 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

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