Specifications

Potent 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.

Product Information

Purity:                                       >95%MW:                                          273.24Formula:                                  C13H11N3O4CAS Number:                           19171-19-8Physical State:                         Lyophilized pale-yellow to yellow-brown solidQuantity:                                  1g; 5gSolubility:                                 25 mg/mL in DMSOStorage:                                    Room Temperature

References

1. Lohbeck & Miller (2016) Practical synthesis of a phthalimide-based Cereblon ligand to enable PROTAC development. Bioorg.Med.Chem.Lett. 26 5260 PMID: 276876732. Nanthakumar et al (2015) Dissecting fibrosis: therapeutic insights from the small-molecule toolbox. Nat.Rev.Drug.Discov. 14 693 PMID: 263381553. Lai et al (2016) Modular PROTAC design for the degradation of oncogenic BCR-ABL. Angew.Chem.Int.Ed.Engl.55 807 PMID: 265933774. Winter et al (2015) Phthalimide conjugation as a strategy for in vivo target protein degradation. Science. 3481376 PMID: 25999370

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