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.
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- Formule: C16H15ClO2Se
- Masse moléculaire:353.70
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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USP30 1.61 μM (Kd) |
GPX4 |
USP30 12.8 μM (IC50) |
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.
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Cell Line:PC3 and DU145 cells
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Concentration:2.5, 5 μM
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Incubation Time:24 h
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Result:Suppressed the invasion capacity of PC3 and DU145 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:25, 50 mg/kg
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Administration:p.o., daily, 18 days
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Result:Achieved significant tumor growth inhibition in male athymic nude mice.
Showed no significant changes in body weight.
Chemical Information
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Masse moléculaire 353.70
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Formule C16H15ClO2Se
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SMILES
ClC(C=CC=C1)=C1[Se]C2=C(C)C3=C(O2)CC(C)CC3=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
USP30-IN-20 Related Classifications
HY-175826 Related Classifications
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