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APY29

A highly potent and selective allosteric modulator of IRE1α
Catalog #: 2591
SKU-Size Size Price Qty
2591-5 5 mg
$85.00
2591-25 25 mg
$335.00
More Sizes Get Quote

Product Details

Alternate Name N2-1H-Benzimidazol-6-yl-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine
Appearance White solid
CAS # 1216665-49-4
Molecular Formula C₁₇H₁₆N₈
Molecular Weight 332.36
Purity ≥98% by HPLC
Solubility DMSO (>30 mg/ml)
SMILES C1(NC2=CC(NC=N3)=C3C=C2)=NC=CC(NC4=NNC(C5CC5)=C4)=N1
InChi InChI=1S/C17H16N8/c1-2-10(1)13-8-16(25-24-13)22-15-5-6-18-17(23-15)21-11-3-4-12-14(7-11)20-9-19-12/h3-10H,1-2H2,(H,19,20)(H3,18,21,22,23,24,25)
InChi Key WJNBSTLIALIIEW-UHFFFAOYSA-N
Handling Protect from light and air
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

APY29 is a highly potent and selective allosteric modulator of IRE1α. Under endoplasmic reticulum (ER) stress, unfolded proteins accumulate in the ER to activate the ER transmembrane kinase/endoribonuclease (RNase)—IRE1α. IRE1α oligomerizes, autophosphorylates, and initiates splicing of XBP1 mRNA, thus triggering the unfolded protein response (UPR). APY29 Inhibits IRE1α autophosphorylation (IC₅₀ = 280 nM) and activates IRE1αRNase activity. As dysregulation of the UPR has been implicated in a variety of cell degenerative and neoplastic disorders, small molecule modulators of IRE1α should be very useful in understanding UPR’s role in pathophysiology and to develop drugs for ER stress-related diseases.


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