CCT007093

Catalog No.S7485 Batch:S748501

Technical Data

Formula

C₁₅H₁₂OS₂

Molecular Weight

272.39

CAS No.

176957-55-4

Solubility (25°C)*

In vitro

DMSO

2.5 mg/mL (9.17 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 Corn oil

1.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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

Targets

PPM1D ^[1]

8.4 μM

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]

Protocol (from reference)

Kinase Assay:^{^[1]}	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 MnCl_{2_{(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 Assay:^{^[1]}	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.

Kinase Assay:^{^[1]}

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 MnCl_{2_{(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 Assay:^{^[1]}

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.

References

Customer Product Validation

: Data from [Data independently produced by , , Oncogene, 2016, 35(42):5552-5564.]

Selleck's CCT007093 has been cited by 1 publication

WIP1 modulates responsiveness to Sonic Hedgehog signaling in neuronal precursor cells and medulloblastoma [Wen J, et al. Oncogene, 2016, 35(42):5552-5564]	PubMed: 27086929

WIP1 modulates responsiveness to Sonic Hedgehog signaling in neuronal precursor cells and medulloblastoma [Wen J, et al. Oncogene, 2016, 35(42):5552-5564]

PubMed: 27086929

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.