APY29 |
Katalog-Nr.GC17139
One-Click Copy Product Info
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APY29, ein ATP-kompetitiver Inhibitor, ist ein allosterischer Modulator von IRE1α, der die Autophosphorylierung von IRE1α durch Bindung an die ATP-Bindungstasche mit einem IC50 von 280 nM hemmt. APY29 fungiert als Ligand, der die benachbarte RNase-DomÄne von IRE1α allosterisch aktiviert.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1216665-49-4
Sample solution is provided at 25 µL, 10mM.
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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.
| 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 |
| Löslichkeit | ≥ 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0088 mL | 15.0439 mL | 30.0879 mL |
| 5 mM | 601.8 μL | 3.0088 mL | 6.0176 mL |
| 10 mM | 300.9 μL | 1.5044 mL | 3.0088 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
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 saline, 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.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)