Home / Pharmacology / Enzymes / Esterases / IRE1 / APY 29

APY 29

Cat. No. 4865 2 Citations Submit a Review Datasheet / COA / SDS
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Description: Inhibits IRE1α autophosphorylation; activates IRE1α endoribonuclease activity
Chemical Name: N2-1H-Benzimidazol-6-yl-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for APY 29

APY 29 is an allosteric modulator of IRE1α. Inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α ribonuclease activity.

Compound Libraries for APY 29

APY 29 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for APY 29

M. Wt 332.36
Formula C17H16N8
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1216665-49-4
PubChem ID 42627755
InChI Key WJNBSTLIALIIEW-UHFFFAOYSA-N
Smiles C1(NC2=CC(NC=N3)=C3C=C2)=NC=CC(NC4=CC(C5CC5)=NN4)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for APY 29

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 33.24 100
1eq. HCl 16.62 50

Preparing Stock Solutions for APY 29

The following data is based on the product molecular weight 332.36. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.01 mL 15.04 mL 30.09 mL
5 mM 0.6 mL 3.01 mL 6.02 mL
10 mM 0.3 mL 1.5 mL 3.01 mL
50 mM 0.06 mL 0.3 mL 0.6 mL

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Product Datasheets for APY 29

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for APY 29

References are publications that support the biological activity of the product.

Wang et al (2012) Divergent allosteric control of the IRE1a endoribonuclease using kinase inhibitors. Nat.Chem.Biol. 8 982 PMID: 23086298

Korennykh et al (2009) The unfolded protein response signals through high-order assembly of Ire1. Nature 457 687 PMID: 19079236

If you know of a relevant reference for APY 29, please let us know.

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2 Citations for APY 29

Citations are publications that use Tocris products. Selected citations for APY 29 include:

Ju-Ri et al (2020) IRE1α kinase-mediated unconventional protein secretion rescues misfolded CFTR and pendrin. Sci Adv 6 eaax9914 PMID: 32128399

Govindarajan et al (2018) Stabilization of cytokine mRNAs in iNKT cells requires the serine-threonine kinase IRE1alpha. Nat Commun 9 5340 PMID: 30559399

Do you know of a great paper that uses APY 29 from Tocris? Please let us know.

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Literature in this Area

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