PPIA-IN-1

PPIA-IN-1 (Compound 20b) is the inhibitor for peptidylprolyl isomerase A (PPIA) with a KD of 0.52 μM. PPIA-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC50 for HCT116 is 0.69 μM), arrests the cell cycle at G0/G1 phase, and exhibits anti-metastatic effect in cell HCT116. PPIA-IN-1 increases ROS, causes DNA damage, ER stress and mitochondrial dysfunction, inducing apoptosis in HCT116 through MAPK pathway. PPIA-IN-1 exhibits antitumor activity in mouse CT26 xenograft models[1].

Product Specifications

CAS Number

[3077886-94-0]

UNSPSC

12352005

Target

Apoptosis; p38 MAPK; Reactive Oxygen Species (ROS)

Related Pathways

Apoptosis; Immunology/Inflammation; MAPK/ERK Pathway; Metabolic Enzyme/Protease; NF-κB

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Purity

96.90

Smiles

O=C(C1(C(OCC)=O)OC(C2=CC=CC=C2F)N3C1N(C(C(OC)=O)=C)C4=NC(Cl)=NC(Cl)=C34)OCC

Molecular Formula

C23H21Cl2FN4O7

Molecular Weight

555.34

References & Citations

[1]Li XJ, et al., Discovery of Novel Oxazolo[4,3-f]purine Derivatives as Antitumor Agents through PPIA Interaction. J Med Chem. 2025 Mar 13;68 (5) :5573-5596.