PROTAC LZK degrader 1

PROTAC LZK degrader 1 (compound 21A) (0.1-10 μM; 24-48 h) binds LZK with a K_d of 35 nM and induces concentration-dependent LZK degradation in Doxycycline (DOX) (HY-N0565)-inducible LZK-overexpressing CAL33 HNSCC cells^[1].
PROTAC LZK degrader 1 (1 μM; 0-48 h) achieves sustained LZK protein depletion over time, accompanied by reduced JNK phosphorylation^[1].
PROTAC LZK degrader 1 (1 μM; 24 h) exerts LZK degradation activity dependent on both proteasome and NEDD8 neddylation pathways, and fully abolishes LZK-degrading activity when co-treated with proteasome inhibitor MG-132 (HY-13259) and NEDD8-activating enzyme inhibitor MLN4924 (HY-70062)^[1].
PROTAC LZK degrader 1 (1 μM; 48 h) downregulates c-MYC and GOF p53 expression in CAL33 cells harboring MAP3K13 amplification^[1].
PROTAC LZK degrader 1 (1-2.5 μM) suppresses colony formation of LZK-amplified CAL33, BICR56, Detroit562 HNSCC cell lines, with minimal toxicity to LZK-wildtype BICR22 and BEAS-2B cells at 1 μM; higher concentration (2.5 μM) induces off-target cytotoxicity in control cells^[1].
PROTAC LZK degrader 1 exerts anti-clonogenic activity via LZK degradation, whereas its cis-epimer only binds LZK without inducing LZK degradation or anti-tumor colony-suppressive function^[1].
PROTAC LZK degrader 1 (100 nM) displays high selectivity toward LZK/DLK across a kinome panel covering over 450 kinases and exhibits negligible off-target kinase inhibitory effects^[1].

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