APY29, IRE1a Modulator


Catalog No. size PriceQuantity
M60168-2S 2 mg solid $109
M60168-10S 10mg solid $441

Description

APY29 is a highly potent and selective small molecule modulator of IRE1α. Under endoplasmic reticulum stress, unfolded protein accumulation leads to activation of the endoplasmic reticulum transmembrane kinase/endoRNase (RNase) IRE1α. IRE1α oligomerizes, autophosphorylates and initiates splicing of XBP1 mRNA, thus triggering the unfolded protein response (UPR). Interestingly, APY29 occupies IRE1α's kinase ATP-binding site to activate RNase-mediated XBP1 mRNA splicing even without upstream endoplasmic reticulum stress. It dose-dependently reduces IRE1α kinase autophosphorylation in vitro with IC50 ~0.28 µM. As dysregulation of the UPR has been implicated in a variety of cell degenerative and neoplastic disorders, small molecule modulators of IRE1α, such as APY29, serve as useful tools to understand the UPR's role in pathophysiology and to develop drugs for endoplasmic reticulum stress-related diseases.

Product information

CAS Number: 1216665-49-4

Molecular Weight: 332.36

Formula: C17H16N8

Chemical Name: N2-(1H-benzo[d]imidazol-6-yl)-N4-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine

Smiles: C1CC1C1=CC(NC2=CC=NC(NC3=CC4NC=NC=4C=C3)=N2)=NN1

InChiKey: WJNBSTLIALIIEW-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

APY29 was used at 2-20 µM in vitro and in cellular assays.

References:

  1. Wang L, et al. Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors. (2012) Nat Chem Biol. 8(12):982-9.
  2. Korennykh AV, et al. The unfolded protein response signals through high-order assembly of Ire1. (2009) Nature. 457(7230):687-93.

Products are for research use only. Not for human use.

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