PD98059

カタログ番号 T2623 CAS 167869-21-8

別名: PD 98059

PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.

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PD98059, CAS 167869-21-8

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
5 mg	在庫あり	￥ 8,000
10 mg	在庫あり	￥ 11,000
25 mg	在庫あり	￥ 17,500
50 mg	在庫あり	￥ 25,000
100 mg	在庫あり	￥ 43,000
200 mg	在庫あり	￥ 64,000
500 mg	在庫あり	￥ 107,500
1 mL * 10 mM (in DMSO)	在庫あり	￥ 12,500

バルクのお問い合わせ

バッチを選択

純度: 100%

COA DATASHEET SDS HNMR HPLC

純度: 99.66%

COA DATASHEET SDS HPLC HNMR

純度: 98.56%

COA DATASHEET SDS LCMS HNMR HPLC

純度: 98.52%

COA DATASHEET SDS HNMR HPLC

COA DATASHEET SDS HNMR

COA DATASHEET SDS

COA DATASHEET SDS HNMR

バッチの詳細情報はお問い合わせください

生物学的特性に関する説明

化学的特性

保存条件 & 溶解度情報

説明	PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.
ターゲット＆IC50	MEK2:50 μM (cell free), MEK1:2 μM (cell free)
In vitro	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. [1] 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. [2]
In vivo	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. [3] 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. [4]
キナーゼ試験	c-Raf and MEK kinase were measured by their ability to activate MAPKK1 (or MAPKK2) in a 30-min coupled assay containing MAPKK1 (or MAPKK2) and its substrate p42 MAP kinase. One unit of c-Raf or MEK kinase activity was that amount which increased the activity of p42Graphic by 1 unit/min. MAPKK was assayed directly in the cell lysate by the activation of bacterially expressed p42Graphic. One unit of MAPKK was that amount which increased the activity of p42Graphic by 1 unit/min. The assays of c-Raf and MAPKK are quantitative and extremely sensitive and are detailed elsewhere. p42Graphic was assayed by its ability to phosphorylate myelin basic protein and MAPKAP kinase 1 α/β by the phosphorylation of a peptide related to the C terminus of ribosomal protein S6 [Gly-245, Gly-246]S6-(218-249). One unit of p42Graphic or MAPKAP kinase-1α/β was that amount which catalyzed the phosphorylation of 1 nmol of substrate peptide in 1 min. Protein kinase activities in immunoprecipitates were measured by adding the other assay components to the tubes containing the immunoprecipitated enzyme [1].
細胞研究	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 [2].
動物実験	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 [4].

別名	PD 98059
分子量	267.28
分子式	C16H13NO3
CAS No.	167869-21-8

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

Ethanol: 1.3 mg/mL (5 mM)

DMSO: 13.75 mg/mL (51.44 mM), Sonication is recommended.

参考文献

1. Zhao Y, et al. MEK inhibitor, PD98059, promotes breast cancer cell migration by inducing β-catenin nuclear accumulation. Oncol Rep. 2017 Nov;38(5):3055-3063. 2. Chen S, et al. Reversing multidrug resistance in hepatocellular carcinoma cells by inhibiting extracellular signal-regulated kinase/mitogen-activated protein kinase signaling pathway activity. Oncol Lett. 2014 Nov;8(5):2333-2339. 3. Di Paola R, et al. PD98059, a specific MAP kinase inhibitor, attenuates multiple organ dysfunction syndrome/failure (MODS) induced by zymosan in mice. Pharmacol Res. 2010 Feb;61(2):175-87. 4. Ahmad SF, et al. MAP kinase inhibitor PD98059 regulates Th1, Th9, Th17, and natural T regulatory cells in an experimental autoimmune encephalomyelitis mouse model of multiple sclerosis. Eur J Pharmacol. 2023 Nov 15;959:176086. 5. Yeh H T, Tsai Y S, Chen M S, et al. Flavopereirine induces cell cycle arrest and apoptosis via the AKT/p38 MAPK/ERK1/2 signaling pathway in human breast cancer cells[J]. European Journal of Pharmacology. 2019: 172658. 6. Chen M S, Lin W C, Yeh H T, et al. Propofol specifically reduces PMA-induced neutrophil extracellular trap formation through inhibition of p-ERK and HOCl[J]. Life sciences. 2019 Mar 15;221:178-186. 7. Hu, Qiuhui, Hengjun Du, Gaoxing Ma, Fei Pei, Ning Ma, Biao Yuan, Paul A. Nakata, and Wenjian Yang. Purification, identification and functional characterization of an immunomodulatory protein from Pleurotus eryngii [J]. Food Funct. 2018 Jul 17;9(7):3764-3775. 8. Chen M S, Yeh H T, Li Y Z, et al. Flavopereirine Inhibits Autophagy via the AKT/p38 MAPK Signaling Pathway in MDA-MB-231 Cells[J]. International Journal of Molecular Sciences. 2020, 21(15): 5362. 9. Zheng Y, Wang Y, Zhang X, et al. C19, a C-terminal peptide of CKLF1, decreases inflammation and proliferation of dermal capillaries in psoriasis[J]. Scientific Reports. 2017 Oct 24;7(1):13890. 10. Dong L, Gong J, Wang Y, et al. Chiral geometry regulates stem cell fate and activity[J]. Biomaterials. 2019: 119456.

引用文献

1. Xu X, Song L, Li Y, et al.Neurotrophin-3 promotes peripheral nerve regeneration by maintaining a repair state of Schwann cells after chronic denervation via the TrkC/ERK/c-Jun pathway.Journal of Translational Medicine.2023, 21(1): 1-20. 2. Zou X, Zeng M, Zheng Y, et al.Comparative Study of Hydroxytyrosol Acetate and Hydroxytyrosol in Activating Phase II Enzymes.Antioxidants.2023, 12(10): 1834. 3. Urade R, Chang W T, Ko C C, et al.A fluorene derivative inhibits human hepatocellular carcinoma cells by ROS-mediated apoptosis, anoikis and autophagy.Life Sciences.2023: 121835. 4. Liu Y, Yuan C, Zhou M, et al. Co-cultured Bone-marrow Derived and Tendon Stem Cells: Novel Seed Cells for Bone Regeneration. Open Life Sciences. 2019, 14(1): 568-575 5. Chen M S, Yeh H T, Li Y Z, et al. Flavopereirine Inhibits Autophagy via the AKT/p38 MAPK Signaling Pathway in MDA-MB-231 Cells. International Journal of Molecular Sciences. 2020, 21(15): 5362 6. Li P, Lin Q, Sun S, et al. Inhibition of cannabinoid receptor type 1 sensitizes triple-negative breast cancer cells to ferroptosis via regulating fatty acid metabolism. Cell Death & Disease. 2022, 13(9): 1-15. 7. Dong L, Gong J, Wang Y, et al. Chiral geometry regulates stem cell fate and activity. Biomaterials. 2019: 119456. 8. Su J W, Li S F, Tao J J, et al. Estrogen protects against acidosis-mediated articular chondrocyte injury by promoting ASIC1a protein degradation. European Journal of Pharmacology. 2021: 174381. 9. Hu Q, Du H, Ma G, et al. Purification, identification and functional characterization of an immunomodulatory protein from Pleurotus eryngii. Food & Function. 2018, 9(7): 3764-3775 10. Chen M S, Tung Y W, Hu C L, et al. Three Lipid Emulsions Reduce Staphylococcus aureus-Stimulated Phagocytosis in Mouse RAW264. 7 Cells. Microorganisms. 2021, 9(12): 2479.

11. Chen M S, Lin W C, Yeh H T, et al. Propofol specifically reduces PMA-induced neutrophil extracellular trap formation through inhibition of p-ERK and HOCl. Life Sciences. 2019 Mar 15;221:178-186 12. Li S, Deng G, Su J, et al. A novel all-trans retinoic acid derivative regulates cell cycle and differentiation of myelodysplastic syndrome cells by USO1. European Journal of Pharmacology. 2021: 174199. 13. Liu Z, Yang J. Uncarboxylated osteocalcin promotes osteogenic differentiation of mouse bone marrow–derived mesenchymal stem cells by activating the Erk‐Smad/β‐catenin signalling pathways. Cell Biochemistry and Function. 2019 14. Chen M S, Yang K S, Lin W C, et al. Lipofundin mediates major inhibition of intravenous propofol on phorbol myristate acetate and Escherichia coli-induced neutrophil extracellular traps. Molecular Biology Reports. 2022: 1-13 15. Yeh H T, Tsai Y S, Chen M S, et al. Flavopereirine induces cell cycle arrest and apoptosis via the AKT/p38 MAPK/ERK1/2 signaling pathway in human breast cancer cells. European Journal of Pharmacology. 2019, 863: 172658 16. Zheng Y, Wang Y, Zhang X, et al. C19, a C-terminal peptide of CKLF1, decreases inflammation and proliferation of dermal capillaries in psoriasis. Scientific Reports. 2017, 7(1): 1-11 17. Yang Z, Guo D, Zhao J, et al.Aggf1 Specifies Hemangioblasts at the Top of Regulatory Hierarchy via Npas4l and mTOR-S6K-Emp2-ERK Signaling.Arteriosclerosis, Thrombosis, and Vascular Biology.2023

もっと見る隠し

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PD98059 167869-21-8 Autophagy Immunology/Inflammation MAPK ERK Aryl Hydrocarbon Receptor MEK AhR Extracellular signal regulated kinases MAP2K MAPKK inhibit Mitogen-activated protein kinase kinase Inhibitor PD-98059 PD 98059 inhibitor

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

PD98059

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords