SJFα
Chemical Name: N-(3-Fluoro-4-((7-(4-(4-(2-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)butoxy)butoxy)-6-methoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Purity: ≥98%
Biological Activity
SJFα is a potent and selective p38α PROTAC® Degrader (DC50 = 7.16 nM; Dmax = 97.4%). SJFα comprises the multikinase inhibitor foretinib joined by a linker to a VHL ligand. Displays significantly lower potency degradation at p38δ (DC50 = 299 nM). Exhibits no significant degradation of p38β, p38γ or related MAPKs, ERK1/2, or JNK1/2.p38γ antibodies validated for Simple Western™ (automated Western) instruments also available: Catalog # AF1347 and MAB1347.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase.
Smith et al.
Nat.Commun., 2019;10:131
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