Chemical Name: 4-Amino-2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione
Biological ActivityPotent TNF-α inhibitor (IC50 = 13 nM). Also potently inhibits IL-2 (EC50 = 8 nM). Thalidomide derivative. Binds cereblon and inhibits its ubiquitination. Exhibits antiproliferative effects in a Namalwa lymphoma cell line. Antiangiogenic. Promotes degradation of transcription factor SALL4.
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.
Practical synthesis of a phthalimide-based cereblon ligand to enable PROTAC development.
Lohbeck and Miller
Dissecting fibrosis: therapeutic insights from the small-molecule toolbox.
Nanthakumar et al.
Modular PROTAC design for the degradation of oncogenic BCR-ABL.
Lai et al.
Phthalimide conjugation as a strategy for in vivo target protein degradation.
Winter et al.
Thal. promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray Syndrome.
Donovan et al.
Evolution of cereblon-mediated protein degradation as a therapeutic modality.
Chamberlain et al.
ACS Med.Chem.Lett., 2019;10:1592
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