PROTAC NAMPT Degrader-31

PROTAC NAMPT Degrader-31 (A13) potently inhibits NAMPT enzymatic activity in a cell-free system with an IC₅₀ of 15 nM^[1].
PROTAC NAMPT Degrader-31 induces potent, concentration- and time-dependent NAMPT degradation in MDA-MB-231 cells (DC₅₀ = 9.31 nM) and 4T1 cells (DC₅₀ = 12.54 nM), with maximum degradation efficiency over 90%^[1].
PROTAC NAMPT Degrader-31 (24 h) dose-dependently reduces intracellular NAD⁺ levels in MDA-MB-231 and 4T1 cells via the NAMPT pathway, with effects at 10 nM reversible by exogenous NMN supplementation^[1].
PROTAC NAMPT Degrader-31 potently inhibits proliferation of MDA-MB-231, 4T1, HCC1937, and BT-549 TNBC cells with IC₅₀ values ranging from 10.29 nM to 32.20 nM, and exhibits over 600-fold selectivity over normal MCF-10A cells; its antiproliferative effects are reversible by exogenous NMN^[1].
PROTAC NAMPT Degrader-31 (10 nM) significantly inhibits migration and invasion of MDA-MB-231 and 4T1 TNBC cells, with effects reversible by exogenous NMN supplementation^[1].
PROTAC NAMPT Degrader-31 (10 nM; 48 h) indirectly induces polarization of cocultured RAW264.7 macrophages toward an M1-like phenotype by degrading NAMPT in 4T1 and MDA-MB-231 TNBC cells, as evidenced by increased CD86 expression, reduced CD206 expression, and elevated M1-associated cytokine levels^[1].

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