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Submit ReviewPD 98059 is an inhibitor of mitogen-activated protein kinase kinase (MKK / MEK). Acts by binding to the inactivated form of MEK, thereby preventing its phosphorylation by cRAF or MEK kinase (IC50 = 2-7 μM). Inhibits cell growth and proliferation in acute myelogenous leukemia (AML) cell lines; causes G1 arrest by blocking p53-dependent p21 induction. Enhances embryonic stem cell self-renewal.
PD 98059 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
分子量 | 267.28 |
公式 | C16H13NO3 |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 167869-21-8 |
PubChem ID | 9794588 |
InChI Key | PKDHDJBNEKXCBI-UHFFFAOYSA-N |
Smiles | COC1=C(N)C(=CC=C1)C1=CC(=O)C2=CC=CC=C2O1 |
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 | 6.68 | 25 | |
ethanol | 1.34 | 5 |
以下数据基于产品分子量 267.28。 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 |
---|---|---|---|
0.25 mM | 14.97 mL | 74.83 mL | 149.66 mL |
1.25 mM | 2.99 mL | 14.97 mL | 29.93 mL |
2.5 mM | 1.5 mL | 7.48 mL | 14.97 mL |
12.5 mM | 0.3 mL | 1.5 mL | 2.99 mL |
参考文献是支持产品生物活性的出版物。
Alessi et al (1995) PD 98059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. J.Biol.Chem. 270 27489 PMID: 7499206
Dudley et al (1995) A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc.Natl.Acad.Sci.U.S.A. 92 7686 PMID: 7644477
Kojima et al (2007) Mitogen-activated protein kinase kinase inhibition enhances nuclear proapoptotic function of p53 in acute myelogenous leukemia cells. 67 3210 PMID: 17409429
Tsang et al (1998) Effects of mitogen-activated protein kinase kinase inhibitor PD 98059 on antigen challenge of guinea-pig airways in vitro. Br.J.Pharmacol. 125 61 PMID: 9776345
Qi et al (2004) BMP4 supports self-renewal of embryonic stem cells by inhibiting mitogen-activated protein kinase pathways. Proc.Natl.Acad.Sci.USA 101 6027 PMID: 15075392
If you know of a relevant reference for PD 98059, please let us know.
关键词: PD 98059, PD 98059 supplier, Specific, inhibitors, inhibits, MEK, MKK, Mitogen-Activated, Protein, Kinase, Kinases, PD98059, stem, cells, Stem, Cell, Proliferation, 1213, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PD 98059 的部分引用包括:
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Cultured mouse neuron treated with PD 98059 (10uM) for 15 mins. MAP staining showed after treatment.
We investigate the effect of LPA on microglia metabolic states. Trying to unravel possible pathways that maybe involved in this process, we used inhibitors of MAPKs pathway. Inhibition of ERK (PD 98059; 10µM) decreased the LPA induced activation of pAMPK (among other proteins).
The role of MAPK pathways (JNK, p38 and ERK) was studied in the LPA induced pro-inflammatory phenotype in microglia. In this case cells were incubated for the indicated time points with LPA (1µM) in the presence or absence of PD98059 (10µM) or PD184352 (10µM). A series of assays were performed. Inhibition of ERK pathway didn't seem to play a role in the LPA induced phenotype (here presented: pp65).
HL-1 cells were incubated with p38 MAPK inhibitor (10 µM SB203580, 25 µMPD169316) or p42/44 MAPK kinase inhibitor (25 µM PD98059) for 30 min prior to 15dPGJ2 treatment (15 µM, 1 h). Immunoreactive bands for pp38 and pp42/44 MAPK expressions were followed by Western blot. PD98059 completely inhibited 15d-PGJ2 induced p42/44 phosphorylation (shown in Image).
Used to treat mouse ovarian theca cells to inhibit MEK and detected by Western blot.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*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.