dWBP4-1

dWBP4-1 (6 h) potently induces degradation of HiBiT-tagged WBP4 in MOLT-4 cells, with a DC₅₀ of 3.4 nM^[1].
dWBP4-1 (100 nM; 0.5-6 h) rapidly and dose-dependently induces the degradation of endogenous WBP4 in MOLT-4 cells, and this degradation effect depends on CRBN and the ubiquitin-proteasome pathway^[1].
dWBP4-1 (1 μM; treatment for 1-24 h with 1 h pretreatment of Cycloheximide (HY-12320)) accelerates the degradation kinetics of endogenous WBP4 in HEK293T cells, and reduces the protein half-life when combined with Cycloheximide^[1].
The CRBN-dependent degradation of endogenous WBP4 mediated by dWBP4-1 (1-1000 nM; 6 h) in HEK293T cells is strictly dependent on CRBN^[1].
dWBP4-1 (1 μM; 6 h) exhibits excellent whole-proteome selectivity in MOLT-4 cells, as it specifically degrades WBP4 at a concentration of 1 μM without altering the levels of other IMiD targets or spliceosome proteins^[1].
dWBP4-1 binds directly and specifically to CRBN with an IC₅₀ of 378 nM^[1].
dWBP4-1 induces the formation of the CRBN-dWBP4-1-WBP4 ternary complex, with an EC₅₀ value of 224 nM^[1].
Degradation of WBP4 induced by dWBP4-1 (6 h) in MOLT-4 cells depends on the G-loop region of the WW1 domain of WBP4, as the WBP4^G146N mutation abolishes efficient degradation^[1].
dWBP4-1 (1-10 μM) induces degradation of the WBP4 truncation-EGFP fusion protein in HEK293T cells, and a 41-amino-acid wTAG sequence serves as the minimal functional degron^[1].
dWBP4-1 (0.17-10000 nM; 1-24 h) induces rapid, potent and monotonic degradation of N-terminal and C-terminal wTAG-fused BRD4-BD1 and PLK1 in HEK293T cells, with DC₅₀ values ranging from 1.4 nM to 31 nM, and no hook effect is observed^[1].

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