USP30 Inhibitor
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CMPD-39
0 ImagesCMPD-39 is a selective non-covalent inhibitor of the ubiquitin-specific protease USP30 (IC50=~20 nM), with high selectivity over other DUB family members (1-100 μM). CMPD-39 inhibits the deubiquitinating activity of USP30, enhances the ubiquitination of mitochondrial proteins TOMM20 and SYNJ2BP; thus, CMPD-39 promotes phosphoubuitin accumulation, thereby accelerating mitochondrial autophagy (mitophagy) and peroxisomal autophagy (pexophagy). CMPD-39 significantly restores impaired mitochondrial function in dopaminergic neurons derived from Parkinson's disease patients.
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Q14
0 ImagesCat. No.: HY-P10416Purity: 98.51%Synonyms: Q14 peptideQ14 is a polypeptide derived from the USP30 (ubiquitin specific peptidase 30) transmembrane (TM) domain with the ability to inhibit the deubiquitination activity of USP30 (IC50=57.2 nM). Q14 reduces USP30 activity by inhibiting the interaction between the USP30 transmembrane domain and its catalytic domain. Q14 peptide contains the LC3 interaction region (LIR) motif, which enables it to bind to the LC3 and accelerate the formation of autophagosomes, thereby promoting mitophagy. Q14 can be used in the study of neurodegenerative diseases as well as mitochondrial quality control and cell metabolism.
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USP30-IN-2
0 ImagesCat. No.: HY-182553CAS No.: 2414580-72-4USP30-IN-2, a fused pyrroline, is an USP30 inhibitor with an IC50 <0.1 μM. USP30-IN-2 is expected to promote mitophagy and restore mitochondrial health. USP30-IN-2 can be used for research on Parkinson's disease.
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MT16-001
0 ImagesCat. No.: HY-182636CAS No.: 1895049-73-6MT16-001 is a cell-permeable UCHL1 inhibitor with an IC50 value of 580 nM. MT16-001 also exhibits considerable inhibitory activity against USP30, and shows selectivity for other UCH family deubiquitinases (DUBs) as well as the broader proteome. MT16-001 binds covalently to the cysteine residue at the active site of UCHL1, and forms covalent interactions with ALDH2, ALDH9A1 and GATD3A in intact cells. Meanwhile, as a cytotoxic agent, it displays a steep dose-response curve in human embryonic kidney cells. MT16-001 can be used for research on various cancers, liver fibrosis and pulmonary fibrosis.
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USP30-IN-1
0 ImagesUSP30-IN-1 is a potent and selective USP30 inhibitor, with IC50 values of 94 nM and 4 nM in vivo and in vitro, respectively, and Ki values of 0.33 μM (Krippendorf method) and 0.38 μM (traditional method), respectively. USP30-IN-1 covalently binds to the catalytic cysteine (Cys77) of USP30, blocks ubiquitin substrate binding to inhibit deubiquitination, and ultimately induces mitophagy. USP30-IN-1 can be used for the research of idiopathic Parkinson's disease and mitophagy-related diseases.
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USP30-IN-20
0 ImagesCat. No.: HY-175826USP30-IN-20 is an orally active USP30 inhibitor (Kd = 1.61 μM, IC50 = 12.8 μM). USP30-IN-20 induces ferroptosis by promoting ubiquitination-mediated degradation of GPX4. USP30-IN-20 inhibits the proliferation, migration, invasion, and stemness of prostate cancer cells. USP30-IN-20 induces G0/G1 cell cycle arrest and ROS levels in prostate cancer cells. USP30-IN-20 exhibits significant anti-tumor efficacy in PC3 cell subcutaneous xenografts in mice. USP30-IN-20 can be used for the study of advanced prostate cancer.
