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Submit ReviewPD 198306 is a potent inhibitor of MEK1/2. Inhibits isolated enzyme at a concentration of 8 nM and inhibits MEK activity in synovial fibroblasts at concentrations of 30 - 100 nM. Highly selective for MEK; IC50 values are > 1, > 4, > 4 and > 10 μM for ERK, c-Src, cdks and PI 3-kinase γ respectively. Antihyperalgesic; blocks static allodynia in the streptozocin model of neuropathic pain following i.t. administration.
分子量 | 476.23 |
公式 | C18H16F3IN2O2 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 212631-61-3 |
PubChem ID | 9956637 |
InChI Key | UHAXDAKQGVISBZ-UHFFFAOYSA-N |
Smiles | CC1=C(NC2=C(C=C(F)C(F)=C2F)C(=O)NOCC2CC2)C=CC(I)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 47.62 | 100 | |
ethanol | 47.62 | 100 |
以下数据基于产品分子量 476.23。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.1 mL | 10.5 mL | 21 mL |
5 mM | 0.42 mL | 2.1 mL | 4.2 mL |
10 mM | 0.21 mL | 1.05 mL | 2.1 mL |
50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
参考文献是支持产品生物活性的出版物。
Ciruela et al (2003) Identification of MEK1 as a novel target for the treatment of neuropathic pain. Br.J.Pharmacol. 138 751 PMID: 12642375
Pelletier et al (2003) In vivo selective inhibition of mitogen-activated protein kinase kinase 1/2 in rabbit experimental osteoarthritis is associated with a reduction in the development of structural changes. Arthrit.Rheumat. 48 1582
If you know of a relevant reference for PD 198306, please let us know.
关键词: PD 198306, PD 198306 supplier, Selective, inhibitors, inhibits, MEK1/2, Mitogen-Activated, Protein, Kinase, kinases, PD198306, MEK, 2605, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PD 198306 的部分引用包括:
Ripple et al (2013) Acute mitochondrial inhibition by mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK) 1/2 inhibitors regulates proliferation. J Biol Chem 288 2933 PMID: 23235157
Liddell et al (2016) Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes. J Neuroinflammation 13 49 PMID: 26920699
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平均评分: 5 (Based on 1 Review.)
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*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.