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CCT007093

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

CCT007093 Chemical Structure

CCT007093 Chemical Structure

CAS: 176957-55-4

Selleck's CCT007093 has been cited by 1 Publication

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Purity & Quality Control

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

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Biological Activity

Description CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM.
Targets
PPM1D [1]
8.4 μM
In vitro
In vitro CCT007093 selectively and potently inhibits human tumor cell lines (MCF-7, KPL-1, and MCF-3B) that overexpress PPM1D. CCT007093 induces cell death via the activation of p38 kinase activity. [1] CCT007093 in combination with paclitaxel, results in synergistic inhibition of the four paclitaxel-resistant triple-negative breast cancer (TNBC) cell lines. [2] CCT007093 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. [3]
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.
Cell Research Cell lines MCF-7, KPL-1, and MCF-3B cells
Concentrations ~50 μM
Incubation Time 14 days
Method Cells are transfected with a pSUPER plasmid and an additional plasmid expressing the blasticidin resistance gene (pEFBsd) in a molar ratio of 10:1. Cells are plated in 10 cm plates 24 h after transfection. Blasticidin selection (5 μg/ml) is initiated 48 h post-transfection and replenished every 3 days. Colonies are fixed in methanol and stained with crystal violet after 14 days. Colonies are quantified on a Colcount and the surviving fraction (SF) determined.

Chemical Information & Solubility

Molecular Weight 272.39 Formula

C15H12OS2
CAS No. 176957-55-4 SDF Download CCT007093 SDF
Smiles C1CC(=CC2=CC=CS2)C(=O)C1=CC3=CC=CS3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 2.5 mg/mL ( (9.17 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

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Tech Support

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.

Handling Instructions

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