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NJH-2-057

Chemical Structure : NJH-2-057

CAS No.: 2858812-70-9

NJH-2-057 (DUBTAC NJH-2-057)

Catalog No.: PC-72837Not For Human Use, Lab Use Only.

NJH-2-057 is a novel CFTR DUBTAC via linking the OTUB1 recruiter EN523 to the CFTR chaperone lumacaftor with C5 alkyl linkers.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

NJH-2-057 is a novel CFTR DUBTAC via linking the OTUB1 recruiter EN523 to the CFTR chaperone lumacaftor with C5 alkyl linkers.
NJH-2-057 robustly stabilizes ΔF508-CFTR protein levels, leading to improved chloride channel conductance in human cystic fibrosis bronchial epithelial cells.
Deubiquitinase-targeting chimeras (DUBTACs), heterobifunctional small molecules consisting of a deubiquitinase recruiter linked to a protein-targeting ligand, to stabilize the levels of specific proteins degraded in a ubiquitin-dependent manner.

Physicochemical Properties

M.Wt 810.856
Formula C43H44F2N6O8
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

N-(5-(3-(5-(4-acryloyl-2-oxopiperazin-1-yl)furan-2-yl)propanamido)pentyl)-3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropane-1-carboxamido)-3-methylpyridin-2-yl)benzamide

References

1. Henning NJ, et al. Nat Chem Biol. 2022 Feb 24. doi: 10.1038/s41589-022-00971-2.

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