GW5074
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GW5074是一种合成的c-Raf抑制剂,其IC50值为9 nM[1].
GW5074是有效的c-Raf抑制剂,对cdk1\cdk2\c-src\p38MAP激酶\VEGFR2以及c-fms无效.GW5074对JNK蛋白以及p38 MAP激酶也无直接作用.在神经元中,GW5074减少c-Raf第259位丝氨酸的磷酸化水平,从而激活c-Raf.实验进一步证明,在剂量低于1 μM时,GW5074显示神经保护作用.此外,GW5074延缓Akt磷酸化的下调,防止GSK3β活化,从而抑制细胞凋亡.在亨廷顿氏病体内模型中,GW5074抑制3-NP诱导的纹状体神经变性,从而保护神经元[1].
我们的产品是ZE构型混合物.
参考文献:
[1] Burgess S, Echeverria V. Raf inhibitors as therapeutic agents against neurodegenerative diseases. CNS & Neurological Disorders-Drug Targets (Formerly Current Drug Targets-CNS & Neurological Disorders), 2010, 9(1): 120-127.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 520.94 |
Cas No. | 220904-83-6 |
Formula | C15H8Br2INO2 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥21.9 mg/mL in DMSO |
Chemical Name | 3-(3,5-dibromo-4-hydroxybenzylidene)-5-iodoindolin-2-one |
SDF | Download SDF |
Canonical SMILES | IC1=CC=C(NC(C2=CC3=CC(Br)=C(O)C(Br)=C3)=O)C2=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
小脑颗粒神经元 |
溶解方法 |
该化合物在DMSO中的溶解度大于26.1 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
1 μM,40 min |
应用 |
用GW5074处理神经元导致c-Raf激活,刺激Raf-MEK-ERK通路。GW5074处理神经元增加B-Raf的活性。GW5074抑制颗粒细胞和其他神经元类型中神经毒素引起的细胞死亡。 |
动物实验 [1,2]: | |
动物模型 |
具有亨廷顿氏病(HD)的C57BL/6雄性小鼠,每天反复暴露在四支烟造成的烟雾环境中的小鼠,暴露4周 |
给药剂量 |
腹腔注射,2 mg/kg,每天给药,三周 |
应用 |
GW5074(5 mg/kg)完全阻止了C57BL/6雄性小鼠中3-NP诱导的大面积双侧纹状体损伤。GW5074(0.5 mg/kg或2 mg/kg)抑制小鼠的侧流烟雾引起的气道高反应性。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Chin P C, Liu L, Morrison B E, et al. The c‐Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK‐ERK and Akt‐independent mechanism[J]. Journal of neurochemistry, 2004, 90(3): 595-608. [2]. Lei Y, Cao Y X, Xu C B, et al. The Raf-1 inhibitor GW5074 and dexamethasone suppress sidestream smoke-induced airway hyperresponsiveness in mice[J]. Respiratory research, 2008, 9(1): 71. |
Description | GW5074是有效的c-Raf选择性抑制剂,其IC50值为9 nM. | |||||
靶点 | C-Raf | |||||
IC50 | 9 nM |
质量控制和MSDS
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