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12147
PD184352
Activators & Inhibitors
Chemical Modulators

PD184352 #12147

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PD184352: Image 1
Western blot analysis of extracts from HeLa cells, serum-starved overnight and untreated or treated with TPA #4174 (200 nM, 20 min) either with or without PD184352 pretreatment (1 hr) at the indicated concentrations, using Phospho-p44/42 MAPK (Erk1/2) (Thr202/Tyr204) (D13.14.4E) XP® Rabbit mAb #4370 (upper) or p44/42 MAPK (Erk1/2) (137F5) Rabbit mAb #4695 (lower).
PD184352: Image 2
Chemical structure of PD184352.

Product Usage Information

PD184352 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1044.6 µl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.1-10 µM for 0.5-1 hr prior to treating with a stimulator or is used alone with varying treatment times lasting up to 24 hr. Soluble in DMSO at 25 mg/ml and ethanol at 8 mg/ml with warming; poorly soluble in water with maximum solubility in water at ~5-10 µM.

Storage

Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight 478.66 g/mol
Purity >99%
Molecular Formula C17H14ClF2IN2O22
CAS 212631-79-3
Solubility Soluble in DMSO at 50mg/ml and EtOH at 8.3mg/ml.

Background

PD184352 (CI-1040) is a highly potent and selective noncompetitive MEK inhibitor with an IC50 of 17 nM for MEK1 (1). Treatment of cells with PD184352 leads to suppression of MAPK activation (1-4) and potently inhibits the proliferation of cells harboring the B-Raf mutation V600E (2,3). Researchers have shown that PD184352 effectively inhibits MEK5, although not as potently as MEK1 (4).
  1. Sebolt-Leopold, J.S. et al. (1999) Nat Med 5, 810-6.
  2. Liu, D. et al. (2007) J Clin Endocrinol Metab 92, 4686-95.
  3. Solit, D.B. et al. (2006) Nature 439, 358-62.
  4. Mody, N. et al. (2001) FEBS Lett 502, 21-4.

Limited Uses

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Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not For Use In Diagnostic Procedures.
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To Purchase # 12147
Cat. # Size Qty. Price
12147S
5 mg
$ 115