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APY29 inhibited IRE1α autophosphorylation (IC50 = 280 nM) and activated IRE1α ribonucase activity. Even in the absence of upstream ER stress, APY29 occupies the kinase ATP-binding site of IRE1α and activates RNASE-mediated SPLicting of XBP1 mRNA. In vitro inhibition of IRE1α kinase autophosphorylation by IC50 ~0.28 μM was dose-dependent.
| Molecular Weight | 332.36 |
| Formula | C17H16N8 |
| CAS Number | 1216665-49-4 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related IRE1 Products |
|---|
| 4μ8C
4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM. |
| STF-083010
STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress. STF-083010 is a potent inhibitor of the ER transmembrane protein IRE1, which mediates the unfolded protein response. |
| KIRA6
KIRA6 is a potent type II IRE1α kinase inhibitor with an IC50 of 0.6 µM. |
| MKC-3946
MKC-3946 is a potent IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines. |
| Kira8
Kira8 (AMG-18) is a single selective IRE1α inhibitor with an IC50 of 5.9 nM. |
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