| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
CCT007093, a thienylidene cyclopentanone, is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM. The PPM1D gene is aberrantly amplified in a range of common cancers and encodes a protein phosphatase that is a potential therapeutic target. CCT007093 shows a potent inhibition of PPM1D in an in vitro assay when using the recombinant phospho-P38 as a substrate. In cellular assay, CCT007093 shows specificity for MCF-7 cells over HeLa cells. It reduces 40% viability of the cells after 2 days. It is found that the cell death induced by CCT007093 is dependent on P38 kinase activity. CCT007093 mimics the effect of PPM1D RNAi in activating P38 kinase.
| ln Vitro |
The phosphorylation levels of mTOR at Ser2448, Ser2481, and Ser2159 are dramatically increased by CCT007093 (25 or 50 µM, 8 h). In transfected HEK293T cell line, the phosphorylation levels of p70S6K (Thr389) and S6 (Ser235/236) are also up-regulated [1]. CCT007093 exhibits selectivity for MCF-7 cells, causing a 40% reduction in viability after two days but having no discernible impact on HeLa cell growth[2]. In MCF-7 cells, which are sensitive to PPM1D inhibition, CCT007093 causes P38 phosphorylation four hours after exposure. In HeLa cells, which are comparatively resistant to PPM1D inhibition, P38 phosphorylation is not induced by CCT007093[2].
|
|---|---|
| ln Vivo |
Mice undergoing major hepatectomy have a higher survival rate and more liver regeneration after receiving CCT007093 (6.4 mg/kg)[1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: HEK293T cell line. Tested Concentrations: 25 or 50 µM. Incubation Duration: 8 h. Experimental Results: The phosphorylation levels of mTOR at Ser2448, Ser2481 and Ser2159 were all Dramatically increased[1]. The phosphorylation levels of p70S6K (Thr389) and S6 (Ser235/236) were also up-regulated[1]. |
| Animal Protocol |
Animal/Disease Models: Wild-type mice[1].
Doses: 3.2 and 6.4 mg/kg. Route of Administration: Injected intraperitoneally 4 times (mice were sacrificed at 36 h post-PH). Experimental Results: Dramatically improved survival in mice following major hepatectomy (80% hepatectomy). The level of PCNA was also Dramatically increased in the liver of CCT007093-treated mice at 36h, 48h and 72h post-PH. |
| References |
[1]. Lingling Zhang, et al. Inhibition of wild-type p53-induced phosphatase 1 promotes liver regeneration in mice by direct activation of mammalian target of rapamycin. Hepatology. 2015 Jun;61(6):2030-41.
[2]. S Rayter, et al. A chemical inhibitor of PPM1D that selectively kills cells overexpressing PPM1D. Oncogene. 2008 Feb 14;27(8):1036-44. |
| Molecular Formula |
C15H12OS2
|
|
|---|---|---|
| Molecular Weight |
272.39
|
|
| CAS # |
176957-55-4
|
|
| Related CAS # |
|
|
| SMILES |
O=C1/C(CC/C1=C\C2=CC=CS2)=C/C3=CC=CS3
|
|
| Chemical Name |
|
|
| Synonyms |
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6712 mL | 18.3560 mL | 36.7121 mL | |
| 5 mM | 0.7342 mL | 3.6712 mL | 7.3424 mL | |
| 10 mM | 0.3671 mL | 1.8356 mL | 3.6712 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|---|
|
Analysis of drug combinations on growth of breast cancer cells grown in 3D cultures.Breast Cancer Res.2010;12(3):R41. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
