- 商品介绍
- 规格参数
- 包装参数
General description
A cell-permeable pyridine-containing vinylogous cyanamide compound that acts as a potent and selective inhibitor of MEK (IC50 = 12 nM) with little activity towards MKK3 and MKK4 (IC50 >1 µM). The inhibition is noncompetitive with respect to ERK and the compound displays significant affinity only towards ATP-bound MEK (i.e. noncompetitive with respect to ATP). Exhibits superior potency, solubility, and stability compared to U0126 (Cat. No. 662005) in aqueous solutions. Shown to protect against phorbol ester-mediated ear edema in mice (ED50 of 5 mg/kg, ip.).
A cell-permeable, potent, and selective inhibitor of MEK (IC50 = 12 nM) with little activity towards MKK3 and MKK4 (IC50 >1 µM). The inhibition is non-competitive with respect to ERK and the compound displays significant affinity only towards ATP-bound MEK (i.e. non-competitive with respect to ATP). Exhibits superior potency, solubility, and stability compared to U0126 (Cat. No. 662005) in aqueous solutions. Shown to protect against phorbol ester-mediated ear edema in mice (ED50 of 5 mg/kg, ip.).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MEK
Product does not compete with ATP.
Reversible: no
Target IC50: 12 nM against MEK
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Wityak, J., et al. 2004. Bioorg. Med. Chem. Lett.14, 1483.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥95% (sum of two isomers, HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | white |
| solubility | DMSO: 10 mg/mL,methanol: 50 mg/mL |
| shipped in | wet ice |
| storage temp. | −20°C |
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¥ 2290.21
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¥ 1259.40
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¥ 2013.69
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¥ 9207.92
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¥ 4968.78
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¥ 6330.00
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¥ 1476.00
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