Antibodies
PD318088
- 貨號 Cat. No.
- S1568
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
PD318088
PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. | |||||
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| Targets | MEK1/2 | |||||
| IC50 | ||||||
| In vitro | PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure. [1] | |||||
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Protocol(Only for Reference)
References
Chemical Information
| Molecular Weight (MW) | 561.09 |
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| Formula | C16H13BrF3IN2O4 |
| CAS No. | 391210-00-7 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 112 mg/mL (199 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 14 mg/mL (24 mM) | ||
| * <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. | |||
| Chemical Name | 5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)benzamide |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.56109 | 5.6109 | 11.2218 | 16.8327 |
Customer Reviews (1)
 Click to enlarge | Rating | |
| Source | Dr. Zhang of Tianjin Medical University. PD318088 purchased from Selleck | |
| Method | Western blot | |
| Cell Lines | A549 cells | |
| Concentrations | 0-10 μM | |
| Incubation Time | 3 h | |
| Results | PD318088 decreased protein expression levels of ERK1/2, but had no effect on ERK1/2 phosphorylation. |
