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G-6599

Chemical Structure : G-6599

CAS No.: 2901806-51-5

G-6599 (G6599)

Catalog No.: PC-25679Not For Human Use, Lab Use Only.

G-6599 is a potent, specific small-molecule SMARCA2/A4 PROTAC degrader with DC50 of 17 pM and 57 pM respectively (SW1573 cells, 20 h, Dmax=95%), acting via the recruitment of FBXO22.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

G-6599 is a potent, specific small-molecule SMARCA2/A4 PROTAC degrader with DC50 of 17 pM and 57 pM respectively (SW1573 cells, 20 h, Dmax=95%), acting via the recruitment of FBXO22.
G-6599 is specific to SMARCA2/A4 and operates through the ubiquitin-proteasome pathway.
G-6599 induces cell growth inhibition comparable to A947 or FHD-286 based on studies in two SMARCA4-mutant models, NCI-H1944 and HCC515, wth no effect on cell growth in NCI-H522 cells that lack SMARCA2/A4.
FBXO22 ligase activity is required for SMARCA2/A4 degradation.
G-6599 acts as a monovalent degrader by covalently targeting FBXO22.

 

Physicochemical Properties

M.Wt 523.69
Formula C31H37N7O
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
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Phenol, 2-[6-amino-5-[8-[2-[4-(hexahydro-1H-azepin-1-yl)-1-butyn-1-yl]-4-pyridinyl]-3,8-diazabicyclo[3.2.1]oct-3-yl]-3-pyridazinyl]-

References

1. Villemure E, et al. Nat Commun. 2025 Nov 3;16(1):9679.

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