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G6374

Chemical Structure : G6374

CAS No.:

G6374 (G-6374)

Catalog No.: PC-25906Not For Human Use, Lab Use Only.

G6374 is a selective, effective PROTAC degrader for endogenous IRE1 with DC50 of 0.04 uM and Dmax of 93% in AMO1 multiple myeloma (MM) cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

G6374 is a selective, effective PROTAC degrader for endogenous IRE1 with DC50 of 0.04 uM and Dmax of 93% in AMO1 multiple myeloma (MM) cells.
G6374 induced effective depletion of IRE1 in KMS27 MM cells, which express similarly high IRE1 levels, with a Dmax of 98% and a DC50 of 0.13 μM.
G6374 promotes stable association between IRE1 and VHL, and drives IRE1 degradation.
G6374 selectively inhibits IRE1-dependent cancer-cell proliferation regardless of the underlying dependency mode.

Physicochemical Properties

M.Wt 883.17
Formula C47H66N10O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S,4R)-4-hydroxy-1-((S)-2-(5-(4-((1r,4S)-4-((8-isopropyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)cyclohexyl)piperazin-1-yl)pentanamido)-3,3-dimethylbutanoyl)-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

References

1. Du J, et al. Nat Commun. 2025 Dec 11. doi: 10.1038/s41467-025-66382-8.

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