HIPK2-IN-2

HIPK2-IN-2 (AF-1) effectively inhibits HIPK2 with an IC₅₀ of 0.36 μM, and exhibits significantly improved selectivity for HIPK2 compared to the closely related HIPK1 (IC₅₀ = 18.41 μM) and HIPK3 (IC₅₀ = 23.32 μM) isoforms^[1].
HIPK2-IN-2 (1-5 μM; 48 h) exhibits low cytotoxicity against NRK-49F cells, with an IC₅₀ of 2.28 μM when cells are stimulated with 10 ng/mL TGF-β₁^[1].
HIPK2-IN-2 (5 μM; 24 h) directly binds to endogenous HIPK2 protein in TGF-β1-stimulated NRK-49F cells and HK-2 human proximal tubular epithelial cells, and this effect is confirmed by the increased thermal stability of HIPK2 following compound exposure^[1].
HIPK2-IN-2 (1-5 μM; 24 h) inhibits TGF-β/Smad3-mediated profibrotic signaling and reduces the expression of fibrotic markers in TGF-β1-stimulated human HK-2 renal tubular epithelial cells; it also blocks the NF-κB inflammatory signaling pathway^[1].
HIPK2-IN-2 (1-2 μM; 10-14 days) effectively inhibits the colony-forming proliferation capacity of TGF-β1-stimulated NRK-49F cells^[1].

HIPK2-IN-2 (2.5-5 μM; 24 h) effectively blocks the migration of TGF-β1-stimulated NRK-49F fibroblasts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.