ITK degrader 1

MedChem Express

ITK degrader 1

10

Research Use Only

C48H57F3N10O7

943.02

ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice), with good plasma exposure levels. ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 consists of target protein ligand (red part) ITK ligand 1 (HY-168387), PROTAC linker (black part) Piperidine-C2-piperazine-Boc (HY-168388) and E3 ubiquitinase ligand (blue part) Thalidomide 5-fluoride (HY-W087383). E3 ubiquitinase and PROTAC linker can form Thalidomide-piperidine-C2-piperazine-Boc (HY-168389)[1].

O=C(NC1=CN([C@@H](CCN2CCN(CCC3CCN(C4=CC=C(C(N(C5CCC(NC5=O)=O)C6=O)=O)C6=C4)CC3)CC2)C7=CC=CC=C7)N=C1)C8=NNC9=C8CCC(C)(C)C9.OC(C(F)(F)F)=O

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