USP30-IN-1
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 番号: 2511541-78-7
- 分子式: C17H15N5O2
- 分子量:321.33
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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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.
化学情報
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CAS 番号 2511541-78-7
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分子量 321.33
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)