XRF-1021

XRF-1021 is an orally active HIPK2 inhibitor (IC50 = 0.18 μM) . XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease[1].

Product Specifications

CAS Number

[2968523-32-0]

UNSPSC

12352005

Target

DYRK; MDM-2/p53; NF-κB; Notch; TGF-beta/Smad; Wnt; β-catenin

Related Pathways

Apoptosis; Neuronal Signaling; NF-κB; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt; TGF-beta/Smad

Field of Research

Inflammation/Immunology

Smiles

NC1=NC2=CC=CC=C2N1C3=NC=C(F)C(NC4=CC=C(N5CCNCC5)C=C4)=N3

Molecular Formula

C21H21FN8

Molecular Weight

404.44

References & Citations

[1]Hu X, et al. Discovery of XRF-1021, a 2,4-disubstituted-5-fluoropyrimidine derivative as a homeodomain-interacting protein kinase 2 inhibitor for the treatment of chronic kidney disease. Eur J Med Chem. 2026 Jan 15;302 (Pt 2) :118353.