MS143

MS143 (compound 20) exhibits the highest affinity for AKT1, moderate affinity for AKT3, and lower affinity for AKT2, with corresponding K_d values of 26 nM, 88 nM, and 400 nM^[1].
MS143 (1 nM-10 μM; 24 h) potently induces concentration-dependent degradation of total AKT in PC3 cells, with a DC₅₀ of 46 nM^[1].
MS143 (1 μM; 1-24 h) induces rapid AKT degradation and inhibits downstream signaling pathways in PC3 cells, with significant degradation achieved within 4 h and complete depletion within 8 h at the concentration of 1 μM^[1].
MS143 (1 μM; 24 h following 2 h pretreatment) induces AKT degradation in PC3 cells in a manner dependent on the VHL E3 ligase and the ubiquitin-proteasome system, which is confirmed by experiments showing that specific pathway inhibitors and competitors restore AKT levels^[1].
MS143 (administered for 5 consecutive days) potently inhibits the proliferation of PC3 and MDA-MB-468 cancer cells, with GI₅₀ values of 0.8 μM and 1.0 μM in the two cell lines, respectively^[1].
MS143 (100 nM-1 μM) exhibits significantly greater selectivity for the degradation of AKT1 and AKT3 over AKT2 in PC3 cells, and depletes approximately 90% of AKT1/AKT3 at a concentration of 100 nM^[1].
MS143 (1 μM; 24 h, followed by washout periods) induces sustained AKT degradation and downstream signaling pathway inhibition in PC3 cells, with only partial recovery of AKT levels observed 48 h after compound washout^[1].
MS143 (1 μM-10 μM; 24 h) potently induces AKT degradation and downstream signaling pathway inhibition in BT474 cells, and effectively suppresses colony formation of this cell line^[1].

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