PD-98059

SKU: orb1305254

特色

描述

PD98059 is a non-ATP-competitive MEK1/2 inhibitor (IC50=2/50 µM) and an aryl hydrocarbon receptor (AHR) antagonist that also suppresses autophagy. It is widely used in vitro to study MAPK/ERK signaling, toxicology, and autophagic pathways in cancer and cellular stress research.

研究领域

Stem Cell & Developmental Biology

图片与验证

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关键属性

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CAS 号	167869-21-8
MW	267.29
纯度	>98%
分子式	C₁₆H₁₃NO₃
SMILES	COc1cccc(c1N)-c1cc(=O)c2ccccc2o1
靶点	Kinase
溶解性	Soluble in DMSO (up to 6 mg/ml).

生物活性

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靶点 IC50	C6 cells:4.2 μM\|MEK2:50 μM\|HT29 cells:4 μM\|MEK1:2 μM (cell free)
体内	METHODS: To test the effect on non-infectious shock, PD98059 (10 mg/kg) was administered intraperitoneally to CD mice with yeast polysaccharide-induced non-infectious shock. RESULTS: Treatment with PD98059 significantly reduced systemic toxicity, weight loss and mortality induced by yeast polysaccharide. METHODS: To investigate the effects on experimental autoimmune encephalitis (EAE), PD98059 (5 mg/kg) was administered intraperitoneally once daily for two weeks to the SJL/J mouse model of EAE. RESULTS: PD98059 corrected immune dysfunction in EAE mice, which occurred concomitantly with the modulation of multiple signaling pathways.
体外	METHODS: Human breast cancer cells MCF-7 and MDA-MB-231 were treated with PD98059 (1-50 μM) for 12-72 h. Cell viability was detected using MTT. RESULTS: PD98059 dose-dependently and time-dependently inhibited the enhancement of breast cancer tumor cells. METHODS: Multidrug-resistant tumor cells SMMC7721/ADM and BEL7402/ADM were treated with PD98059 (2.5-20 μM) for 1 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: PD98059 down-regulated pERK1/2 expression in cells in a dose-dependent manner.
细胞研究	The MCF10A-Neo and MCF10A-NeoT lines were derived by transfection of the MCF10A cell line with the pHo6 plasmid and the pHo6 plasmid containing an Ha-ras oncogene derived from the human T24 bladder carcinoma cell line, and subsequent selection for resistance to G418. The transfected lines represent pooled survivors, as opposed to clonal lines. With the exception of the EGF content being increased from 10 to 20 ng/ml, the cells were cultured in supplemented Dulbecco's modified Eagle's medium/Ham's F-12 medium in a humidified atmosphere of 95% air/5% CO2 at 37°C. Subconfluent cultures were treated with varying concentrations of chemicals dissolved in DMSO (absolute volume of solvent < 0.1% of medium volume). Subconfluent cultures are treated with PD98059 (0-100 μM). Viability of cells after treatment was assessed by ability to exclude trypan blue. Cultures earmarked for RNA isolation were washed twice with phosphate-buffered saline (2.7 mM KCl, 1.5 mM KH2PO4, 137mM NaCl, 8 mM Na2HPO4, pH 7.2) at harvesting and stored at 280°C .
动物研究	Mice were randomized into 4 groups (n= 40 animals/group): (i) CAR + vehicle group. Mice were subjected to carrageenan-induced pleurisy and received the vehicle for PD98059 (10% dimethylsulfoxide (DMSO) (v/v) i.p. bolus 1 h after carrageen administration(N=10); (ii) PD98059 group. Same as the CAR + vehicle group but were administered PD98059 (10 mg/kg, i.p. bolus) 1 h after carrageenan administration (N=10); (iii) Sham+saline group. Sham-treated group in which identical surgical procedures to the CAR group were performed, except that the saline was administered instead of carrageenan (n=10); (iv) Sham+ PD98059 group. Identical to Sham+saline group except for the administration of PD98059 (10 mg/kg i.p. bolus) 1h after carrageenan administration of saline (N=10). The doses of PD98059 (10 mg/kg) used here were based on previous in vivo studies that demonstrated regulation of the inflammation process .

储存与操作

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储存	RT
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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2’-Amino-3’-methoxyflavone

相似产品

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PD98059 [orb1225975]
纯度：
>98% (HPLC)
CAS 号：
167869-21-8
MW:
267.2793
分子式：
C₁₆H₁₃NO₃
可选规格： 5 mg, 500 mg, 1 g, 10 mg, 50 mg, 100 mg, 200 mg
PD-98059 [orb3066681]
可选规格： 25 mg, 5 mg

质量保证

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化合物标识

PubChem CID

4713 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

纯度：	>98% (HPLC)
CAS 号：	167869-21-8
MW:	267.2793
分子式：	C₁₆H₁₃NO₃

PD-98059

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

PD98059 [orb1225975]

PD-98059 [orb3066681]

质量保证

化合物标识

关键属性

实验方案信息

可选规格