PROTAC RNF4 degrader-1

PROTAC RNF4 degrader-1 (Compound RD12) (0.2-20 μM; 72 h) potently inhibits the proliferation of HepG2 human hepatocellular carcinoma cells with an IC₅₀ of 0.48 μM^[1].
PROTAC RNF4 degrader-1 (0.1-10 μM; 6 h) induces dose-dependent degradation of RNF4 protein in HepG2 human hepatocellular carcinoma cells^[1].
PROTAC RNF4 degrader-1 (0-20 μM; 6 h) induces dose-dependent degradation of RNF4 protein in Huh7 human hepatocellular carcinoma cells with a DC₅₀ of 4.16 μM^[1].
PROTAC RNF4 degrader-1 (5 μM; 6 h after 2 h pre-incubation with MG132)-mediated RNF4 degradation in HepG2 and Huh7 human hepatocellular carcinoma cells is dependent on the ubiquitin-proteasome system, as pre-treatment with proteasome inhibitor MG132 reverses RNF4 loss^[1].
PROTAC RNF4 degrader-1 (0.1-10 μM; 6 h) induces dose-dependent DNA damage in HepG2 and Huh7 human hepatocellular carcinoma cells, as measured by increased γH2AX levels^[1].
PROTAC RNF4 degrader-1 (0-20 μM; 6 h) increases levels of RNF4 substrate proteins BRCA1 and MDC1 in a dose-dependent manner in Huh7 human hepatocellular carcinoma cells, consistent with RNF4 degradation^[1].
PROTAC RNF4 degrader-1 (serial two-fold dilutions; 30 min at room temperature) binds directly to recombinant RNF4 protein with a K_d of 64.5 nM, as measured by MST^[1].
PROTAC RNF4 degrader-1 (10 μM; 6 h) selectively induces degradation of RNF4 in Huh7 human hepatocellular carcinoma cells, with only 28 of 7483 identified proteins showing significant down-regulation^[1].
PROTAC RNF4 degrader-1 (5 μM; 48 h) induces apoptosis in 52.1% of Huh7 human hepatocellular carcinoma cells^[1].

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