FPA 124 (Synonyms: Akt Inhibitor XI) |
| カタログ番号GC17984 |
細胞透過性銅錯体である FPA 124 は、IC50 が 0.1 μM の選択的 Akt 阻害剤です。 FPA 124 は、プレクストリン相同性 (PH) と Akt のキナーゼ ドメインの両方と相互作用します。 FPA 124 はアポトーシスを誘導します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 902779-59-3
Sample solution is provided at 25 µL, 10mM.
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The kinase Akt (also known as protein kinase B or PKB) modulates cell proliferation, metabolism, and survival, as well as angiogenesis.[1],[2] Akt inhibitor XI is a cell-permeable, copper-containing 3-formylchromone derivative that inhibits Akt in an array of cancer cells (IC50s = 10-34 µM).[3] It also causes NF-κB inactivation in an orthotopic pancreatic tumor model using COLO 357 cells.3 Molecular modeling indicates that this inhibitor interacts with the pleckstrin homology and kinase domains of Akt. Akt inhibitor XI is commonly used in the range of 1-20 µM to assess the role of Akt in cellular responses.[4],[5],[6]
Reference:
[1]. Manning, B.D., and Cantley, L.C. AKT/PKB signaling: Navigating downstream. Cell 129(7), 1261-1274 (2007).
[2]. Yuan, T.L., and Cantley, L.C. PI3K pathway alterations in cancer: Variations on a theme. Oncogene 27(41), 5497-5510 (2008).
[3]. Barve, V., Ahmed, F., Adsule, S., et al. Synthesis, molecular characterization, and biological activity of novel synthetic derivatives of chromen-4-one in human cancer cells. Journal of Medicinal Chemistry 49(13), 3800-3808 (2006).
[4]. Frampton, G., Invernizzi, P., Bernuzzi, F., et al. Interleukin-6-driven progranulin expression increases cholangiocarcinoma growth by an Akt-dependent mechanism. Gut 61(2), 268-277 (2012).
[5]. Rybchyn, M.S., Slater, M., Conlgrave, A.D., et al. An Akt-dependent increase in canonical Wnt signaling and a decrease in sclerostin protein levels are involved in strontium ranelate-induced osteogenic effects in human osteoblasts. The Journal of Biological Chemisty 286(27), 23771-23779 (2011).
[6]. Zareen, N., Biswas, S.C., and Greene, L.A. A feed-forward loop involving Trib3, Akt and FoxO mediates death of NGF-deprived neurons. Cell Death and Differentiation 20(12), 1719-1730 (2013).
| Cas No. | 902779-59-3 | SDF | |
| 同義語 | Akt Inhibitor XI | ||
| Chemical Name | copper(II) (Z)-2-((4-oxo-4H-chromen-3-yl)methylene)hydrazinecarbimidothioate chloride hydrochloride | ||
| Canonical SMILES | N=C([S-])N/N=C([H])\C1=COC2=CC=CC=C2C1=O.[Cl-].Cl.[Cu+2] | ||
| Formula | C11H9Cl2CuN3O2S | M.Wt | 381.73 |
| 溶解度 | DMSO: 0.1 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6197 mL | 13.0983 mL | 26.1965 mL |
| 5 mM | 523.9 μL | 2.6197 mL | 5.2393 mL |
| 10 mM | 262 μL | 1.3098 mL | 2.6197 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
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.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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