GXF-111

GXF-111 (compound 24) binds to BRD3 BD2 with high affinity (K_i = 2.45 nM) and shows lower affinity for BRD3 BD1 (K_i = 11.97 nM), exhibiting approximately 5-fold selectivity for the BD2 domain of BRD3^[1].
GXF-111 (3-4) potently inhibits the growth of MV4-11 and MM.1S cells, with IC₅₀ values of 6.31 nM and 95.2 nM after 3-day and 4-day treatment, respectively^[1].
GXF-111 (for 4 days) inhibits the growth of MCF-7 (IC₅₀ = 0.23 μM), HGC-27 (IC₅₀ = 2.35 μM), A549 (IC₅₀ = 14.26 μM), HeLa (IC₅₀ = 6.96 μM) and HepG2 (IC₅₀ = 17.25 μM) cells^[1].
GXF-111 (0.1-30 nM; 24 h) selectively degrades BRD3 (1-3 nM) and BRD4-L in MM.1S cells without affecting BRD4-S, and only exerts a partial effect on BRD2 at higher doses; meanwhile, this compound regulates the expression of c-Myc and p21 without inducing significant apoptosis^[1].
GXF-111 (30 nM; 1-24 h) induces time-dependent selective degradation of BRD3 and BRD4-L in MM.1S, HGC-27 and MCF-7 cells. Compared with BRD2, the degradation of BRD3/BRD4-L initiates earlier, and GXF-111 exerts minimal effects on BRD4-S within 24 hours^[1].
GXF-111 (0.1-1000 nM; 24 h) selectively degrades BRD3 and BRD4-L (but not BRD2 or BRD4-S) in HGC-27, MCF-7, A549, HeLa and HepG2 cells, while it selectively degrades BRD4-L and BRD4-S in MV4-11 cells; its degradation efficacy varies among different cell lines^[1].
The degradation of BRD3 and BRD4-L in MM.1S cells induced by GXF-111 (30 nM; 4 h) depends on its binding to BET proteins, binding to Cereblon, and functional proteasome activity^[1].
GXF-111 (1-300 nM; 24 h) induces G₁-phase cell cycle arrest in MM.1S cells in a dose-dependent manner^[1].

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