2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Itk
  5. Itk Degrader

Itk Degrader

Itk Degraders (3):

Cat. No. Product Name Effect Purity
  • HY-149917
    ITK degrader 1
    		Degrader
    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).
  • HY-153322
    ITK degrader 2
    		Degrader
    ITK degrader 2 (compound 30) is an orally active, PROTAC-based ITK-targeted degrader (DC50<10 nM). ITK degrader 2 exhibits Cmax and Tmax in mice (po; 90 mg/kg) of 0.87 μM and 2 h, respectively. At this dose, ITK degrader 2 degrades ITK by 20% (6 h) in mice.
  • HY-101321A
    Immepip dihydrobromide
    		Degrader 99.89%
    Immepip dihydrobromide is a H3 agonist. Immepip dihydrobromide can reduce cortical histamine release. Immepip dihydrobromide can be used for the research of neurological diseases.