PROTAC TTK degrader-1

PROTAC TTK degrader-1 (compound 8e) potently degrades TTK protein in COLO-205 human colorectal cancer cells, with a DC₅₀ of 1.7 nM and a maximum degradation rate of 88% after 6 h of treatment; it also potently degrades TTK protein in HCT-116 human colorectal cancer cells, with a DC₅₀ of 5.8 nM and a maximum degradation rate of 80% after 6 h of treatment^[1].
PROTAC TTK degrader-1 (5-50 nM; 6 h) induces dose-dependent TTK degradation in LOVO, HCT-8 and HCT-29 human colorectal cancer cells; it also induces TTK degradation in COLO-205 human colorectal cancer cells, and this degradation effect persists for 6-8 h after compound washout^[1].
PROTAC TTK degrader-1 (5-50 nM; 6 h) induces TTK degradation in human COLO-205 colorectal cancer cells, and this degradation effect is abolished by simultaneous administration of 5 μM TTK inhibitor 6, verifying that its degradation activity relies on target protein binding^[1].
PROTAC TTK degrader-1 (5-50 nM; 1 h pretreatment followed by 6 h incubation) triggers TTK degradation in human COLO-205 colorectal cancer cells through proteasome-dependent pathways, and pre-treatment with 5 μM MG132 (HY-13259) completely abolishes this TTK degradation effect^[1].
PROTAC TTK degrader-1 (0.000508-10 μM; 96 h) potently inhibits the proliferation of human colorectal cancer cell line COLO-205, with an IC₅₀ of 0.1 μM after 96 h of treatment^[1].

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