| Name | CCT007093 |
| Description | CCT007093 is an effective PPM1D (WIP1) inhibitor (IC50: 8.4 μM). |
| Cell Research | 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.(Only for Reference) |
| 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. |
| In vivo | CCT007093, when used in combination with Paclitaxel, synergistically inhibits four Paclitaxel-resistant triple-negative breast cancer cell lines. CCT007093 selectively exhibits significant inhibition on human tumor cell lines over-expressing PPM1D (MCF-7, KPL-1, and MCF-3B). By activating p38 kinase activity, CCT007093 induces cell death. It selectively promotes apoptosis in breast cancer cells and ectopically expressed Wip1 in keratinocytes, while reducing UV-mediated apoptotic responses in Wip1-deficient naked cells and a skin keratinocyte model. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 1.38 mg/mL (5.07 mM), Sonication is recommended.
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| Keywords | PPM1D | Phosphatase | Inhibitor | inhibit | CCT-007093 | CCT007093 | CCT 007093 | Autophagy | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Hemin | Urea | Tamoxifen | Guanidine hydrochloride | Hydroxychloroquine | Metronidazole | Formamide | Paeonol | Naringin | Alginic acid |
| Related Compound Libraries | Apoptosis Compound Library | Glycometabolism Compound Library | Bioactive Compound Library | Autophagy Compound Library | Multi-Target Compound Library | Inhibitor Library | Metabolism Compound Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max | Phosphatase Inhibitor Library |
United States
