TPST2-IN-1

TPST2-IN-1 is a potent and selective TPST2 inhibitor with an IC50 of 946 nM and a Ka of 19.4 μM. TPST2-IN-1 increases the phosphorylation of Stat1 and upregulates the IFNγ-responsive gene CXCL10 by inhibiting TPST2 activity.TPST2-IN-1 exhibits anti-tumor activity and enhances T cell-mediated antitumor immunity characterized by increased infiltration of effector CD8+ T cells. TPST2-IN-1 can be used for the research of cancer, such as colon cancer[1].

Product Specifications

UNSPSC

12352005

Target

STAT; Transmembrane Glycoprotein

Related Pathways

Immunology/Inflammation; JAK/STAT Signaling; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

O=C(C[C@@H]1CC[C@H](CC1)C2=CC=C(C=C2)N3CCN(CC3)C(CCC(NC4=NC(C5=CC(F)=C(C(F)=C5)O)=CS4)=O)=O)O

Molecular Formula

C31H34F2N4O5S

Molecular Weight

612.69

References & Citations

[1]Park SB, et al. Discovery of (4-Phenyl-cyclohexyl) acetate-Derived Tyrosylprotein Sulfotransferase 2 (TPST2) Inhibitors with Potent Anti-Tumor Activity for Immuno-Oncology Applications. J Med Chem. 2025;68 (21) :22401-22427.