受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C15H8Br2INO2 |
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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) |
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* <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. |
製品説明 | GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. GW5074 inhibits LK-induced apoptosis. |
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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 GW5074 permits accumulation of activating modifications on c-Raf and also B-Raf. The inhibition of LK-induced apoptosis by GW5074 in cerebellar granule neurons is not MEK-ERK-dependent. GW5074 delays down-regulation of Akt activity but inhibits apoptosis by an Akt-independent mechanism. GW5074 affects Ras, nuclear factor-kappa B and c-jun. GW5074 inhibits cell death caused by neurotoxins in granule cells and other neuronal types. [1] |
in vivo | GW5074 is protective in an in vivo experimental model of Huntington’s disease. GW5074 (5 mg/Kg) completely prevented extensive bilateral striatal lesions induced by 3-NP in mice. [1] GW5074 suppresses sidestream smoke-induced airway hyperresponsiveness in mice. [3] |
キナーゼアッセイ | Affinity determination | |
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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, GW5074 is added at the time cortical neurons are exposed to HCA. Viability is assessed 24 h later. |
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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. |
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Data from [Mol Cell Proteomics, 2012, 11, 745-57]
Data from [Mol Cell Proteomics, 2012, 11, 745-57]
, , Oncotarget, 2016, 7(33):53558-53570
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 |
SIRT5-mediated deacetylation of LDHB promotes autophagy and tumorigenesis in colorectal cancer [ Mol Oncol, 2019, 13(2):358-375] | PubMed: 30443978 |
Mitochondrial metabolic reprograming via BRAF inhibition ameliorates senescence. [ Exp Gerontol, 2019, 126:110691] | PubMed: 31421186 |
Comparative analysis of the phototoxicity induced by BRAF inhibitors and alleviation through antioxidants. [ Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520] | PubMed: 31618797 |
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。
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