NU227326

NU227326 (4.5 nM; 24 h) potently degrades IDO1 in U87-HiBit-IDO1 human glioblastoma (GBM) cells, with a DC₅₀ of 4.5 nM and a maximum degradation efficiency of 63%^[1].
NU227326 (0.001-10 μM; 24 h) induces dose-dependent degradation of IDO1 in IFNγ-stimulated human U87 glioblastoma (GBM) cells, with a degradation rate of 88% at 100 nM after 24 h, and a hook effect is observed at higher concentrations^[1].
NU227326 (0.001-10 μM; 24 h) reduces kynurenine production in IFNγ-stimulated human U87 glioblastoma (GBM) cells in a dose-dependent manner, and its inhibitory effect persists despite a hook effect on IDO1 protein levels^[1].
NU227326 (100 nM; 0-24 h) initiates IDO1 degradation between 8 and 16 hours and sustains continuous degradation within 24 hours in IFNγ-stimulated human U87 glioblastoma (GBM) cells^[1].
NU227326 (50-100 nM; 24-72 h) induces persistent degradation of IDO1 in IFNγ-stimulated human U87 glioblastoma (GBM) cells; the effect lasts up to 72 hours with continuous treatment, and persists for 48 hours when cells are subjected to 24-hour pulse treatment followed by 0-48 hours of washout^[1].
NU227326 (100 nM; 24 h) mediates IDO1 degradation in IFNγ-stimulated human U87 glioblastoma (GBM) cells, a process that requires binding to the active site of IDO1, recruitment of the CRL4^CRBN E3 ubiquitin ligase complex, and functional proteasomal activity^[1].
NU227326 (50-100 nM; 24 h) potently and dose-dependently degrades IDO1 in multiple human cancer cell lines stimulated with IFNγ, including glioblastoma multiforme (GBM) models, prostate cancer cells, breast cancer cells, pancreatic cancer cells, and ovarian cancer cells, and this effect occurs after treatment at 50 or 100 nM for 24 h^[1].
NU227326 binds directly to CRBN (K_d = 380 nM) and IDO1 (K_d = 140 nM), and forms a stable ternary complex with IDO1 and CRBN^[1].
NU227326 (1 μM; 24 h) exhibits high selectivity for IDO1 degradation, with only a small number of off-target proteins (ADO, EPHX2, CDK8, SALL4, ITCH) being significantly degraded in Kelly human neuroblastoma cells after treatment with 1 μM for 24 h^[1].

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