Description
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.
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.
Alternate Name/Synonyms: N2-1H-Benzimidazol-6-yl-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine
Appearance: White solid
Formulation: N/A
CAS Number: 1216665-49-4
Structure Available?: Y
Peptide sequence: N/A
Salt Form: No
Molecular Formula: C₁₇H₁₆N₈
Molecular Weight: 332.36
Cell-Permeable?: yes
Purity: ≥98% by HPLC
Solubilities: DMSO (>30 mg/ml)
Handling: Protect from light and air
Country of Origin: USA
Tag Line: A highly potent and selective allosteric modulator of IRE1α
MDL Number: N/A
PubChem CID: N/A
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
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |