Akt3 degrader 1

Akt3 degrader 1 (1000 nM; 24 h) selectively induces proteasomal degradation of Akt3 with a DC₅₀ of 13 nM in Osimertinib (HY-15772)-resistant H1975OR NSCLC cells, while having minimal impact on Akt1 and Akt2^[1].
Akt3 degrader 1 (1.6-1000 nM; 24 h) selectively induces dose-dependent degradation of Akt3 in A549, HCC827, H1975, H1975OR, PC9, H1299, and H460 NSCLC cell lines, with no significant impact on Akt1 or Akt2 levels^[1].
Akt3 degrader 1 (100 nM; 0-12 h) accelerates the degradation of Akt3 protein in Cycloheximide (HY-12320)-treated H1975OR NSCLC cells, reducing Akt3 stability over 12 hours^[1].
Akt3 degrader 1 (100 nM; 24 h)-induced degradation of Akt3 in H1975OR NSCLC cells is mediated by the ubiquitin-proteasome system, as the effect is blocked by co-treatment with the proteasome inhibitor MG132^[1].
Akt3 degrader 1 (3-30 nM; 24 h) dose-dependently increases the ubiquitination of Akt3 in H1975OR NSCLC cells, supporting ubiquitin-mediated proteasomal degradation as the mechanism of action^[1].
Akt3 degrader 1 (50 μM; 2 h) directly binds to Akt3 protein in H1975OR NSCLC cells, as demonstrated by competitive labeling with a chemical probe, pull-down validation, and LC-MS analysis^[1].
Akt3 degrader 1 (2 μM) binds to Akt3 in H1975OR NSCLC cells, as indicated by an increase in Akt3 protein thermal stability^[1].
Akt3 degrader 1 (0-100 nM for H1975OR transfected cells; 0-500 nM for H1975 transfected cells) binds to the PH domain of Akt3 to induce degradation, as it fails to degrade PH domain-deleted Akt3 but effectively degrades PH domain-only Akt3 in H1975OR NSCLC cells, and degrades full-length Akt3 in H1975 NSCLC cells^[1].
Akt3 degrader 1 (12l) (0.000508-10 μM; 72 h) potently suppresses the proliferation of Osimertinib-resistant H1975OR NSCLC cells with an IC₅₀ of 7 nM^[1].

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