1. Cell Cycle/DNA Damage Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Deubiquitinase Ferroptosis Reactive Oxygen Species (ROS) Glutathione Peroxidase
  3. USP30-IN-20

USP30-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.

For research use only. We do not sell to patients.

USP30-IN-20

USP30-IN-20 Chemical Structure

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Description

USP30-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[1].

IC50 & Target[1]

USP30

1.61 μM (Kd)

USP30

12.8 μM (IC50)

In Vitro

USP30-IN-20 (Compound 8m) shows potent anti-proliferative activity against PC3, DU145 prostate cancer cells, and CD24-CD44+ prostate cancer stem-like cells, with IC50 values of 4.87 μM, 5.44 μM, and 5.94 μM, respectively[1].
USP30-IN-20 (2.5-5 μM, 14 days) significantly reduces the number of malignant colonies of PC3 and DU145 cells[1].
USP30-IN-20 (2.5-5 μM, 24-48 h) induces G0/G1 phase arrest, inhibits the migration and suppresses the invasion capacity of PC3 and DU145 cells[1].
USP30-IN-20 (2.5-5 μM, 72 h) disrupts tumor sphere formation and significantly reduces the number of spheroids in PC3 and DU145 cells[1].
USP30-IN-20 (2.5-5 μM, 24 h) significantly upregulates intracellular ROS and lipid ROS levels, increases malondialdehyde (MDA) content and decreases glutathione (GSH) levels in PC3 and DU145 cells[1].
USP30-IN-20 (5 μM, 24 h) causes mitochondrial shrinkage, disappearance of mitochondrial cristae and membrane structure, and disruption of mitochondrial membrane potential in PC3 cells, without affecting cell apoptosis[1].
USP30-IN-20 (2.5-5 μM; 24 h) downregulates GPX4 protein expression in a dose-dependent manner in PC3 and DU145 cells[1].

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

Cell Invasion Assay[1]

Cell Line: PC3 and DU145 cells
Concentration: 2.5, 5 μM
Incubation Time: 24 h
Result: Suppressed the invasion capacity of PC3 and DU145 cells.
In Vivo

USP30-IN-20 (Compound 8m) (25-50 mg/kg, p.o., daily, 18 days) significantly inhibits the proliferation of PC3 prostate cancer xenograft tumors in male athymic nude mice[1].

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

Animal Model: PC3 prostate cancer cells (1 × 107 cells) were subcutaneously implanted into the flanks of 6-8-week-old male athymic nude mice (BALB/c strain)[1]
Dosage: 25, 50 mg/kg
Administration: p.o., daily, 18 days
Result: Achieved significant tumor growth inhibition in male athymic nude mice.
Showed no significant changes in body weight.
Molecular Weight

353.70

Formula

C16H15ClO2Se

SMILES

ClC(C=CC=C1)=C1[Se]C2=C(C)C3=C(O2)CC(C)CC3=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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USP30-IN-20
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HY-175826
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