GW5074

製品コードS2872 バッチS287201

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₅H₈Br₂INO₂

分子量

520.94

CAS No.

220904-83-6

Solubility (25°C)*

体外

DMSO

104 mg/mL (199.63 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	30.000mg/ml (57.59mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	GW5074は、IC50が9 nMの強力で選択的なc-Raf阻害剤であり、JNK1/2/3、MEK1、MKK6/7、CDK1/2、c-Src、p38 MAP、VEGFR2、またはc-Fmsの活性には影響を及ぼしません。GW5074はLK誘導性アポトーシスを阻害します。
in vitro	GW5074 is a potent and specific inhibitor of c-Raf with IC50 of 9 nM and has no effect of MKK6, MKK7, p38 MAP kinase and cdks in vitro. However, treatment of neuronal cultures with this compound permits accumulation of activating modifications on c-Raf and also B-Raf. The inhibition of LK-induced apoptosis by this inhibitor in cerebellar granule neurons is not MEK-ERK-dependent. This chemical delays down-regulation of Akt activity but inhibits apoptosis by an Akt-independent mechanism. It affects Ras, nuclear factor-kappa B and c-jun. This compound inhibits cell death caused by neurotoxins in granule cells and other neuronal types.
in vivo	GW5074 is protective in an in vivo experimental model of Huntington’s disease. This compound (5 mg/Kg) completely prevented extensive bilateral striatal lesions induced by 3-NP in mice. It suppresses sidestream smoke-induced airway hyperresponsiveness in mice.

プロトコル(参考用のみ)

キナーゼアッセイ	Affinity determination
キナーゼアッセイ	In general, in vitro kinase assays are performed using purified kinase and synthetic substrates under standard conditions using the Kinase Profiling service of Upstate Biotechnology. Briefly, for each assay 5–10 mU of purified kinase is used. For GSK3β, cdk1, cdk2, cdk3, cdk5, the kinase is incubated with 1 μM GW5074 in a buffer containing 8 mM MOPS, pH 7.2, 0.2 mM EDTA, 10 mM magnesium acetate and [c- ³³P-ATP] for 40 min at room temperature. Kinase activity is quantified by measuring ³³P incorporation by spotting an aliquot on P30 filters, washing in 50 mM phosphoric acid and scintillation counting. The buffer composition for c-Raf, JNK1, JNK2, JNK3, MEK1, MKK6, MKK7 is 50 mM Tris pH 7.5, 0.1 mM EGTA, 10 mM magnesium acetate and [c- ³³P-ATP]. The peptide substrates used are as follows: For c-Raf, 0.66 mg/mL MBP; for cdks, 0.1 mg/mL histone H1; for JNKs, 3 μM ATF2; for MEK1, 1 μM MAPK2; for MKK6, 1 μM of SAPK2a and for MKK7, 2 μM JNK1α.
細胞アッセイ	細胞株	Cortical neurons
	濃度	~5 μM
	反応時間	24 hours
	実験の流れ	HCA is diluted from 100-fold concentrated solutions that are adjusted to pH 7.5. To evaluate the effects of GW5074 on HCA-induced cytotoxicity, this compound is added at the time cortical neurons are exposed to HCA. Viability is assessed 24 h later.
動物実験	動物モデル	Eight-week-old C57BL/6 male mice administered with 50–55 mg/kg 3-NP
	投薬量	0.5–10 mg/kg
	投与方法	i.p.

参考

http://www.ncbi.nlm.nih.gov/pubmed/?term=15255937
http://www.ncbi.nlm.nih.gov/pubmed/?term=16750187
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2599896/

カスタマーフィードバック

: Data from [Mol Cell Proteomics, 2012, 11, 745-57]

: Data from [Mol Cell Proteomics, 2012, 11, 745-57]

: , , Oncotarget, 2016, 7(33):53558-53570

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Evaluation of a Novel Pan-RAS Inhibitor in 3D Bioprinted Tumor Models [ Cancers (Basel), 2025, 17(18)2958]	PubMed: 41008802
Single-cell RNA sequencing reveals the CRTAC1+ population actively contributes to the pathogenesis of spinal ligament degeneration by SPP1+ macrophage [ Aging Cell, 2024, e14320.]	PubMed: 39158018
Evaluating Novel Combinations of Polyamine Targeting Therapeutics in Pancreatic Ductal Adenocarcinoma [ University of Central Florida, 2022, ]	PubMed: none
Degradation of lipid droplets by chimeric autophagy-tethering compounds [ Cell Res, 2021, 10.1038/s41422-021-00532-7]	PubMed: 34239073
DFMO Improves Survival and Increases Immune Cell Infiltration in Association with MYC Downregulation in the Pancreatic Tumor Microenvironment [ Int J Mol Sci, 2021, 22(24)13175]	PubMed: 34947972
Kinase Inhibitor Library Screening Identifies the Cancer Therapeutic Sorafenib and Structurally Similar Compounds as Strong Inhibitors of the Fungal Pathogen Histoplasma capsulatum [ Antibiotics (Basel), 2021, 10(10)1223]	PubMed: 34680804
Stiffness-mediated mesenchymal stem cell fate decision in 3D-bioprinted hydrogels [ Burns Trauma, 2020, 8:tkaa029]	PubMed: 32733974
Depolarization-Dependent C-Raf Signaling Promotes Hyperexcitability and Reduces Opioid Sensitivity of Isolated Nociceptors after Spinal Cord Injury [ J Neurosci, 2020, 40(34):6522-6535]	PubMed: 32690613
Cigarette smoke induction of S100A9 contributes to chronic obstructive pulmonary disease [ Am J Physiol Lung Cell Mol Physiol, 2020, 10.1152/ajplung.00207.2020]	PubMed: 32964723
Reversal of Infected Host Gene Expression Identifies Repurposed Drug Candidates for COVID-19 [ bioRxiv, 2020, 2020/9/20.4.7.30734]	PubMed: 32511305

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。