PROTAC USP39 Degrader-1

PROTAC USP39 Degrader-1 (compound USP39_PROTAC_V1) reduces the thermal stability of purified full-length USP39 protein, decreasing its melting temperature by 1.5 °C^[1].
PROTAC USP39 Degrader-1 (0.5 nM-5 μM; 24 h) induces dose-dependent degradation of USP39 protein in HEK293T, LNCap and Kelly cells^[1].
PROTAC USP39 Degrader-1 (10 nM-1 µM; 24 h) alters splicing activity in HEK293T cells^[1].
PROTAC USP39 Degrader-1 (1 nM-1 µM; 6-24 h) exerts significant target protein degradation activity in HeLa cells transiently overexpressing USP39-OFP, with the optimal treatment condition being 16 h of serum starvation followed by 24 h of compound treatment^[1].
PROTAC USP39 Degrader-1 (0.5 nM-5 μM; 6 h-24 h) exerts potent activity in degrading endogenous USP39 protein in HeLa-WT cells (with a 24 h DC₅₀ of approximately 1.06 nM). It degrades its target with high specificity across the whole proteome, resulting in significant downregulation of USP39 and stress-related proteins without affecting homologous proteins^[1].
The USP39-degrading effect of PROTAC USP39 Degrader-1 (0.1 nM-0.1 μM; 24 h) is significantly inhibited by the proteasome inhibitor MG132 (HY-13259) in co-treated HeLa-WT cells^[1].
The degradation effect of PROTAC USP39 Degrader-1 (10 nM; 24 h) is blocked by the Neddylation inhibitor MLN4924 (HY-70062) in HeLa-USP39-OFP cells co-treated with 1 μM MLN4924^[1].
When PROTAC USP39 Degrader-1 is co-treated with 5 μM MLN4924 in HeLa-USP39-OFP cells, its DC₅₀ increases from 13 nM to 204 nM, and its degradation activity is significantly attenuated^[1].
PROTAC USP39 Degrader-1 (0.5 nM-0.5 μM) shows significantly attenuated USP39-degrading activity in VHL-knockout HeLa cells, and exhibits potent degrading activity only in the presence of wild-type VHL in HEK293T cells co-expressing USP39-OFP and different VHL plasmids (VHL_WT or truncated VHL_m)^[1].
PROTAC USP39 Degrader-1 (0.5 nM-0.5 μM) promotes the formation of a ternary complex between the target protein and VHL_WT in HEK293T cells transfected with different types of plasmids (K_D = 12 nM), whereas the complex formation is extremely weak in the presence of VHL_m^[1].
PROTAC USP39 Degrader-1 (100 nM; 6 h) significantly enriches USP39 and polyubiquitination, and promotes the binding of USP39 to VHL in HeLa cells co-treated with 10 μM MLN4924^[1].
PROTAC USP39 Degrader-1 (10 nM; 24 h) induces aberrant usage of non-canonical 5'-splice sites in HEK293T cells, recapitulating the splicing defects associated with USP39 depletion^[1].

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