ITK degrader 1
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 , 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).
Product Specifications
UNSPSC
12352005
Target
Itk; PROTACs
Type
Reference compound
Related Pathways
PROTAC; Protein Tyrosine Kinase/RTK
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/itk-degrader-1.html
Solubility
10 mM in DMSO
Smiles
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
Molecular Formula
C48H57F3N10O7
Molecular Weight
943.02
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Frequently Asked Questions
Explore Other Products
Browse additional items from our catalog
Human Enhancer Of Zeste Homolog 1 (EZH1) ELISA Kit
Human Enhancer Of Zeste Homolog 1 (EZH1) ELISA Kit
CD45RB (B-Cell Marker) (PTPRC/2877R), CF647 conjugate, 0.1mg/mL
