2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Deubiquitinase
  5. USP8 Isoform

USP8

Ubiquitin-specific protease 8 (USP8) functions as a deubiquitinating enzyme critical for protein homeostasis by regulating endosomal and lysosomal trafficking[1]. Mechanistically, USP8 stabilizes multiple receptor tyrosine kinases (RTKs) such as EGFR, c-Met, and Kit, thereby influencing downstream signaling pathways that control cell proliferation, survival, and migration[2][1]. In disease models, USP8 mutations or overexpression have been implicated in corticotroph pituitary adenomas and multiple myeloma, promoting tumor growth and therapy resistance[3][1]. Compared with related isoforms like USP7 and USP15, USP8 exhibits specificity for RTK substrates and has distinct effects on plasma and germinal center B-cell populations[4][1]. Inhibition of USP8 using small-molecule inhibitors such as DUB-IN-2 selectively induces degradation of oncogenic RTKs, disrupts proteostasis, and sensitizes resistant cancer cells to proteasome inhibitors[2][1]. These characteristics make USP8 a valuable target for experimental applications in cancer research and endocrine disease studies, allowing mechanistic investigation of deubiquitination-dependent signaling and therapeutic intervention strategies[3][1].

USP8 Related Products (4):

Cat. No. Product Name Effect Purity
  • HY-162312
    LLK203
    		Inhibitor 98.58%
    LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model.
  • HY-151563A
    OTUB1/USP8-IN-1 TFA
    		Inhibitor 99.56%
    OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model.
  • HY-149902
    USP8-IN-3
    		Inhibitor 98.37%
    USP8-IN-3 (Compd U51) is a deubiquitinase USP8 inhibitor with an IC50 value of 4.0 μM. USP8-IN-3 also inhibits the proliferation of GH3 and H1957 cells with GI50s of 37.03 μM and 6.01 μM, respectively.
  • HY-149901
    USP8-IN-2
    		Inhibitor 99.91%
    USP8-IN-2 (Compd U52) is a deubiquitinase USP8 inhibitor with an IC50 value of 6.0 μM. USP8-IN-2 also inhibits the proliferation of H1957 cells with an GI50 value of 24.93 μM, respectively.