PROTAC JAK1/2 degrader-1

PROTAC JAK1/2 degrader-1 (Compound A8) is a selective JAK1/2 PROTAC degrader, with DC50 values of 1.4 μM for JAK1 and 0.92 μM for JAK2. PROTAC JAK1/2 degrader-1 significantly inhibits the release of NO, IL-6 (IC50 = 12.89 μM) and TNF-α (IC50 = 17.17 μM) . PROTAC JAK1/2 degrader-1 significantly alleviates inflammatory responses and colonic damage by inhibiting the JAK/STAT3 signaling pathway. PROTAC JAK1/2 degrader-1 can be used for research on colitis. (Pink: JAK1/2 ligand (HY-179716) ; Blue: CRBN ligand (HY-10984) ; Black: linker; CRBN ligand + linker (HY-131888A) ) [1].

Product Specifications

UNSPSC

12352005

Target

Interleukin Related; JAK; PROTACs; STAT; TNF Receptor

Related Pathways

Apoptosis; Epigenetics; Immunology/Inflammation; JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Field of Research

Inflammation/Immunology

Smiles

O=C(NCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)C4=CC=C(C5=NC(NC6=CC=CC=C6)=NC=C5)C=C4

Molecular Formula

C33H29N7O5

Molecular Weight

603.63

References & Citations

[1]Li G, et al. Development of potent JAK1/2 PROTAC degraders for the treatment of inflammatory bowel diseases. Eur J Med Chem. 2026 Jan 15;302 (Pt 3) :118374.