MT16-001
MT16-001 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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- No. CAS: 1895049-73-6
- Fòrmula: C15H14N4OS
- Peso molecular:298.36
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
USP30 |
ALDH2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
730 nM
Compound: MT16-001
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Cytotoxicity against human HEK293 cells assessed as reduction in cell growth incubated for 72 hrs by live-cell time-lapse imaging
Cytotoxicity against human HEK293 cells assessed as reduction in cell growth incubated for 72 hrs by live-cell time-lapse imaging
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[PMID: 34820624] |
In Vitro
MT16-001 (30 min) potently inhibits recombinant UCHL1 (IC50 = 580 nM) and USP30 at 1 μM, while showing no inhibition of recombinant UCHL3 at concentrations up to 10 μM[1].
MT16-001 (72 h) exhibits cytotoxicity against HEK293 cells with an EC50 of 730 nM[1].
MT16-001 (1 h) engages UCHL1 in intact Cal51 cells stably expressing FLAG-UCHL1 with an IC50 of 550 nM[1].
MT16-001 (2-2000 nM; 3 h) causes no acute disruption of the whole proteome in HEK293 cells at concentrations up to 2000 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1895049-73-6
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Peso molecular 298.36
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Fòrmula C15H14N4OS
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SMILES
O=C([C@@H]1CN(CC1)C#N)NC2=NC=C(C3=CC=CC=C3)S2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MT16-001 Related Classifications
HY-182636 Related Classifications
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