PROTAC JAK2 degrader-1

PROTAC JAK2 degrader-1 (Compound 10i) is a JAK2 PROTAC degrader with a DC50 of 27.35 nM for JAK2 V617F. PROTAC JAK2 degrader-1 promotes the ubiquitination and degradation of JAK2. PROTAC JAK2 degrader-1 inhibits the phosphorylation of JAK2, STAT3 and STAT5. PROTAC JAK2 degrader-1 can be used in the research of myeloproliferative neoplasms (Pink: JAK2 ligand (HY-174430) ; Blue: E3 ligase ligand (HY-W087383) ; Black: E3 ligase ligand + linker (HY-174432) ) [1].

Product Specifications

UNSPSC

12352005

Target

JAK; PROTACs; STAT

Related Pathways

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

Field of Research

Cancer

Smiles

FC1=CC([C@H](OC2=C(N=CC(C3=CN(N=C3)C4CCN(CC4)CC5CN(CC5)CC6CCN(CC6)C7=CC(C(N8C9CCC(NC9=O)=O)=O)=C(C=C7)C8=O)=C2)N)C)=C(C=C1)Cl

Molecular Formula

C45H51ClFN9O5

Molecular Weight

852.40

References & Citations

[1]Wang C, et al. Discovery of a Proteolysis-Targeting Chimera Degrader of JAK2 as a Potential Therapeutic Agent for JAK2-Mediated Myeloproliferative Neoplasms. J Med Chem. 2025 Jun 12;68 (11) :12085-12099.