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CCT007093 phosphatase inhibitor

Cat.No.S7485

CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM.
CCT007093 phosphatase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 272.39

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Quality Control

Batch: S748501 DMSO]2.5 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.08%
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99.08

Solubility

In vitro
Batch:

DMSO : 2.5 mg/mL (9.17 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 272.39 Formula

C15H12OS2

Storage (From the date of receipt)
CAS No. 176957-55-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CC(=CC2=CC=CS2)C(=O)C1=CC3=CC=CS3

Mechanism of Action

Targets/IC50/Ki
PPM1D
8.4 μM
In vitro
CCT007093 selectively and potently inhibits human tumor cell lines (MCF-7, KPL-1, and MCF-3B) that overexpress PPM1D. This compound induces cell death via the activation of p38 kinase activity. It in combination with paclitaxel, results in synergistic inhibition of the four paclitaxel-resistant triple-negative breast cancer (TNBC) cell lines. This chemical selectively promote apoptosis in breast cancer cells and skin transformed keratinocytes that ectopically expressed Wip1, while attenuates the UV-mediated apoptotic response in both skin keratinocytes and a Wip1-null cell model.
Kinase Assay
In vitro phosphatase assay
Recombinant PPM1D (20-50 pmol) is diluted in Tris buffer (50 mM, pH 8), NaCl (100 mM), β-mercaptoethanol (1 mM) or DTT (1 mM) and treated with MnCl2 (0, 1, 10 and 20 mM) or MgCl2 (0 and 40 mM). Where appropriate, inhibitors of PPM1D (10-50 μM) are added and the assay mix incubated for 30 min at room temperature. Recombinant phospho-P38 (200 pmol) is then added and the mixture incubated at 37°C for 1 h. The reaction is quenched by the addition of excess ethylenediaminetetraacetic acid (EDTA), sodium dodecyl sulphate-sample loading buffer and boiling for 5 min at 95°C followed by gel electrophoresis and western blotting.
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