USP30-IN-1
Based on 1 Customer Validation
USP30-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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- CAS. Nr.: 2511541-78-7
- Formel: C17H15N5O2
- Molecular Weight:321.33
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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USP30 94 nM (IC50, in vivo) |
USP30 4 nM (IC50, in vitro) |
USP30-IN-1 (compound USP30-I-1) (0.01-10 μM; 1 h) blocks the binding of the HA-Ub-PA probe to endogenous USP30 in lysates of SH-SY5Y neuroblastoma cells, potently and specifically inhibits USP30 activity, but weakly inhibits USP10 activity[1].
USP30-IN-1 (30 min) dose-dependently inhibits the activity of USP30 in catalyzing the cleavage of ubiquitin-rhodamine substrate in a cell-free system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y neuroblastoma cell lysates
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Concentration:0, 0.01, 0.1, 1, 10 μM
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Incubation Time:1 h
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Result:Dose-dependently inhibited the labeling of endogenous USP30 by HA-Ub-PA, demonstrating highly selective and potent target inhibition.
Chemical Information
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CAS. Nr. 2511541-78-7
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Molecular Weight 321.33
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Formel C17H15N5O2
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SMILES
N#CC1=CC=CC(C2=CN=C(C(N[C@@H]3C[C@@H](C)N(C#N)C3)=O)O2)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (311.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
Verweise
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1121 mL | 15.5603 mL | 31.1207 mL | 77.8016 mL |
| 5 mM | 0.6224 mL | 3.1121 mL | 6.2241 mL | 15.5603 mL | |
| 10 mM | 0.3112 mL | 1.5560 mL | 3.1121 mL | 7.7802 mL | |
| 15 mM | 0.2075 mL | 1.0374 mL | 2.0747 mL | 5.1868 mL | |
| 20 mM | 0.1556 mL | 0.7780 mL | 1.5560 mL | 3.8901 mL | |
| 25 mM | 0.1245 mL | 0.6224 mL | 1.2448 mL | 3.1121 mL | |
| 30 mM | 0.1037 mL | 0.5187 mL | 1.0374 mL | 2.5934 mL | |
| 40 mM | 0.0778 mL | 0.3890 mL | 0.7780 mL | 1.9450 mL | |
| 50 mM | 0.0622 mL | 0.3112 mL | 0.6224 mL | 1.5560 mL | |
| 60 mM | 0.0519 mL | 0.2593 mL | 0.5187 mL | 1.2967 mL | |
| 80 mM | 0.0389 mL | 0.1945 mL | 0.3890 mL | 0.9725 mL | |
| 100 mM | 0.0311 mL | 0.1556 mL | 0.3112 mL | 0.7780 mL |