G-5758 | IRE1α inhibitor | Probechem Biochemicals

Chemical Structure : G-5758

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G-5758 (G5758)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	588.58
分子式	C27H24F4N6O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-Phenyl-N-(2,3,6-trifluoro-4-((3-(2-(((3S,5S)-5-fluoropiperidin-3-yl)amino)pyrimidin-4-yl)pyridin-2-yl)oxy)phenyl)methanesulfonamide

参考文献

1. Braun MG, et al. J Med Chem. 2024 May 15. doi: 10.1021/acs.jmedchem.3c02425.

G-5758 (G5758)

生物&药学活性

物理化学性质&存储条件

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G-5758 (G5758)

生物&药学活性

物理化学性质&存储条件

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