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DHC-156

Chemical Structure : DHC-156

CAS No.:

DHC-156 (DHC156)

Catalog No.: PC-21752Not For Human Use, Lab Use Only.

DHC-156 is a covalent small molecule inhibitor of oncogenic transcription factor brachyury, selectively binds to brachyury, DHC-156 is potent brachyury downmodulator with DC50 of 4.1 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

DHC-156 is a covalent small molecule inhibitor of oncogenic transcription factor brachyury, selectively binds to brachyury, DHC-156 is potent brachyury downmodulator with DC50 of 4.1 uM.
DHC-156 is a chemical analog of afatinib that lacks kinase inhibition activity, whereas afatinib is highly reactive with multiple kinases.
DHC-156 (10 uM) significantly decreased the brachyury fluorescent by immunofluorescent staining of brachyury in CH-22 cells.
DHC-156 downmodulates brachyury post-translationally, displays loss of brachyury phenotyp, results in an irreversible impairment of chordoma tumor cell growth.

Physicochemical Properties

M.Wt 492.47
Formula C24H24F4N4O3
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

(E)-4-(dimethylamino)-N-(1-((4-fluoro-3-(2,2,2-trifluoroethoxy)phenyl)amino)-6-methoxyisoquinolin-7-yl)but-2-enamide

References

1. Chase DH, et al. Angew Chem Int Ed Engl. 2024 Feb 13:e202316496.

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