ZJK-807

ZJK-807 (Compound A11) (10 μM, 0.5-24 h) results in a time-dependent reduction in KRAS^G12D levels and a significant decrease in pERK levels, and can continue to degrade even after it has been removed in AsPC-1 cells^[1].
ZJK-807 (1-3 μM, 12-16 h), at 1 μM for 16 hours, promotes the strong recruitment of HA-KRAS^G12D to CRBN E3 ligase in AsPC-1 cells, proving the formation of ternary complexes, and at 3 μM for 12 hours, it significantly enhances the polyubiquitination of KRAS^G12D in the same cell line^[1].
ZJK-807 (0.1-3 μM, 24 h) induces significant, concentration-dependent degradation of KRAS protein in AsPC-1 (KRAS^G12D) cells, and shows no appreciable degradation of KRAS protein was observed in other KRAS mutant cell lines^[1].
ZJK-807 (1.5-10000 nM, 24 h) exhibits potent and concentration-dependent degradation of KRAS^G12D with DC₅₀ values of 79.5 nM (D_MAX 92%) in AsPC-1 cells, 130.8 nM (D_MAX 92%) in GP2D cells, and 313.8 nM (D_MAX 70%) in AGS cells, while it does not induce concentration-dependent degradation of CK1α or GSPT1 in AsPC-1 and GP2D cells^[1].
ZJK-807 (3 or 5 days) exhibits antiproliferative effects on KRAS^G12D mutant cell lines, with IC₅₀ values of 219.6 nM in AsPC-1, 273.5 nM in AGS, and 1110 nM in GP2D cells, and shows no substantial antiproliferative activity was observed in cell lines with wild-type or other KRAS mutations or on the normal cell line HEK-293T^[1].
ZJK-807 (0.01-10 μM, 24 h) can reduce KRAS^G12D protein levels in a concentration-dependent manner in AGS cells even in the presence of secondary mutations, and although its inhibitory efficacy is reduced, it still inhibits Ba/F3 cells carrying KRAS^G12D/95mut or KRAS^{G12D/96mut [1]}.
ZJK-807 significantly alters the transcriptome with notable down-regulation and pathway enrichment in RAS/MAPK signaling^[1].

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