KH-1

KH-1 binds specifically to purified KRAS^G12D protein with high nanomolar affinity (K_d = 11.63 nM via MST, 8.62 nM via ITC); it also binds to purified HDAC2 protein (K_d = 20.17 nM via MST, 17.14 nM via ITC), which represents its primary HDAC target^[1].
KH-1 exhibits only extremely low off-target inhibitory activity against 330 tested kinases, with an IC₅₀ value > 10 μM^[1].
KH-1 (0.5-12.5 μM; 10 days) potently inhibits the proliferation of human pancreatic cancer Capan-1 (IC₅₀ = 0.49 μM) and PANC-1 cells in a dose-dependent manner, but does not suppress the growth of KRAS^WT, KRAS^G12C, or non-malignant pancreatic epithelial cells^[1].
KH-1 (0.5-12.5 μM; 48 h) potently inhibits the migration and invasion of human pancreatic cancer Capan-1 and PANC-1 cells in a dose-dependent manner^[1].
KH-1 (0.5-12.5 μM) induces dose-dependent apoptosis in human pancreatic cancer Capan-1 and PANC-1 cells; the proportion of apoptotic cells increases, and the expressions of activated caspase-3 and activated poly (ADP-ribose) polymerase are up-regulated; it induces dose-dependent G0/G1 phase arrest in human pancreatic cancer Capan-1 and PANC-1 cells, accompanied by the up-regulation of p-cdc2 expression and the down-regulation of cyclin B1 expression^[1].

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