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Chemical Structure : G-5758
Catalog No.: PC-22293Not For Human Use, Lab Use Only.
G-5758 (G5758) is a potent and selective, orally active IRE1α inhibitor with IC50 of 0.27 nM in HTRF IRE1α binding assays, inhibits IRE1α-Rnase with IC50 of 4.3 nM.
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G-5758 (G5758) is a potent and selective, orally active IRE1α inhibitor with IC50 of 0.27 nM in HTRF IRE1α binding assays, inhibits IRE1α-Rnase with IC50 of 4.3 nM.
G-5758 potently inhibits XBP1 splicing with IC50 of 38 nM in cellular XBP1s luciferase reporter assay.
G-5758 displays 100-fold more selective against 219 kinases and at least 83-fold selective against HIPK4.
G-5758 demonstrated a robust PD response to induced IRE1 knockdown in the sh9/8 KMS-11 xenograft model.
| M.Wt | 588.58 | |
| Formula | C27H24F4N6O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Braun MG, et al. J Med Chem. 2024 May 15. doi: 10.1021/acs.jmedchem.3c02425.
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