ML364

For research use only.

Catalog No.S6748

ML364 Chemical Structure

Molecular Weight(MW): 517.54

ML364 is a small molecule inhibitor of the deubiquitinase USP2 with an IC50 of 1.1 μM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate.

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Biological Activity

Description ML364 is a small molecule inhibitor of the deubiquitinase USP2 with an IC50 of 1.1 μM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate.
Targets
USP8 [1]
(Cell-free assay)
USP2 [1]
(Cell-free assay)
0.95 μM 1.1 μM
In vitro

ML364 induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest in Mino and HCT116 cancer cell lines. ML364 is antiproliferative in cancer cell lines. ML364 also causes a decrease in homologous recombination-mediated DNA repair. It is inactive against caspase 6, caspase 7, MMP1, MMP9, and USP15, but does inhibit USP8 with an IC50 of 0.95 μM. In a panel of 102 kinases that included regulators of the cell cycle there is no binding observed to any of the enzymes tested using 10 μM ML364[1].

Protocol

Cell Research:

[1]

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  • Cell lines: LnCAP cells and MCF7 cells
  • Concentrations: 0-20 μM
  • Incubation Time: 24 h
  • Method:

    ML364 promotes degradation of cyclin D1 in LnCAP cells and MCF7 cells. Cells are treated with ML364 for 24 h, and cyclin D1 protein levels are assessed by Western blotting using a tubulin control.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 50 mg/mL (96.61 mM)
Ethanol 25 mg/mL (48.3 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 517.54
Formula

C24H18F3N3O3S2

CAS No. 1991986-30-1
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CC=C(C=C1)[S](=O)(=O)NC2=CC(=CC=C2C(=O)NC3=NC(=CS3)C4=CC=CC=C4)C(F)(F)F

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID