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ZXH-3-26

Chemical Structure : ZXH-3-26

CAS No.:

ZXH-3-26

Catalog No.: PC-35204Not For Human Use, Lab Use Only.

ZXH-3-26 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC), shows activity exclusively on the BRD4 BD1 (DC50/5h=5 nM) and spares degradation of BRD2 or BRD3 in cellular degradation assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

ZXH-3-26 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC), shows activity exclusively on the BRD4 BD1 (DC50/5h=5 nM) and spares degradation of BRD2 or BRD3 in cellular degradation assays; ZXH-3-26 represents the first small molecule to allow pharmacologic targeting of BRD4 without significant inhibition or degradation of BRD2 and BRD3.

Physicochemical Properties

M.Wt 785.273
Formula C38H37ClN8O7S
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

methyl 2-((6S)-4-(4-chlorophenyl)-2-((5-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)pentyl)carbamoyl)-3,9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate

References

1. Nowak RP, et al. Nat Chem Biol. 2018 Jun 11. doi: 10.1038/s41589-018-0055-y.

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