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Submit ReviewVX 745
说明： Potent and selective p38α inhibitor
别名： VX745,VX-745,Neflamapimod
化学名： 5-(2,6-Dichlorophenyl)-2-[2,4-difluorophenyl)thio]-6H-pyrimido[1,6-b]pyridazin-6-one
纯度： ≥98% (HPLC)
生物活性 for VX 745
VX 745 is a highly potent and selective p38α/MAPK14 inhibitor, also inhibits p38β (IC50 values are 10 nM and 220 nM respectively). VX 745 blocks TNFα production in LPS-stimulated HWB in vitro (IC50 = 51-180 nM). Also reduces phosphorylation of p38MAPKα and the downstream target Hsp27, leading to vasodilation, reduces IL-1β levels and amyloid plaques in cortex and hippocampus and lowers CSF tau levels in vivo.
External Portal Information for VX 745
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of VX 745 is reviewed on the chemical probes website.
化合物库 for VX 745
VX 745 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
技术数据 for VX 745
| 分子量 | 436.26 |
| 公式 | C19H9Cl2F2N3OS |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 209410-46-8 |
| PubChem ID | 3038525 |
| InChI Key | VEPKQEUBKLEPRA-UHFFFAOYSA-N |
| Smiles | O=C2N=CN1N=C(SC4=CC=C(F)C=C4F)C=CC1=C2C3=C(Cl)C=CC=C3Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for VX 745
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 43.63 | 100 |
制备储备液 for VX 745
以下数据基于产品分子量 436.26。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.29 mL | 11.46 mL | 22.92 mL |
| 5 mM | 0.46 mL | 2.29 mL | 4.58 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.29 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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产品说明书 for VX 745
参考文献 for VX 745
参考文献是支持产品生物活性的出版物。
Bagley et al (2007) Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells. Bioorg.Med.Chem.Lett. 17 5107 PMID: 17659871
Goldstein et al (2010) Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. J.Med.Chem. 53 2345 PMID: 19950901
Duffy et al (2011) The discovery of VX-745: a novel and selective p38α kinase inhibitor. ACS Med.Chem.Lett. 2 758 PMID: 24900264
Pandey et al (2022) Neflamapimod induces vasodilation in resistance mesenteric arteries by inhibiting p38 MAPKα and downstream Hsp27 phosphorylation. Sci.Rep. 12 4905 PMID: 35318382
Petrova et al (2020) p38 MAPK signalling regulates cytokine production in IL-33 stimulated type 2 innate lymphoid cells. Sci.Rep. 10 3479 PMID: 32103032
Alam (2015) Selective brain-targeted antagonism of p38 MAPKα reduces hippocampal IL-1 levels and improves Morris Water Maze performance in aged rats. J.Alzheimers Dis. 48 219 PMID: 26401942
If you know of a relevant reference for VX 745, please let us know.
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关键词: VX 745, VX 745 supplier, VX745, p38a, p38alpha, p38α, MAPK14, inhibitors, inhibits, selective, potent, neflamapimod, neurodegeneration, neuroregeneration, vasodilation, amyloid, tau, TNFalpha, TNFα, VX-745, Neflamapimod, p38, 3915, Tocris Bioscience
5 篇 VX 745 的引用文献
引用文献是使用了 Tocris 产品的出版物。 VX 745 的部分引用包括：
Crozier et al (2023) CDK4/6 inhibitor-mediated cell overgrowth triggers osmotic and replication stress to promote senescence. Mol.Cell 83 4062 PMID: 37977118
Ignacio et al (2020) CDK8 Fine-Tunes IL-6 Transcriptional Activities by Limiting STAT3 Resident Time at the Gene Loci. Cell Rep 33 108545 PMID: 33357429
Gerald R et al (2021) Increased ACTL6A occupancy within mSWI/SNF chromatin remodelers drives human squamous cell carcinoma. Mol Cell 81 4964-4978.e8 PMID: 34687603
Singh et al (2018) Differential effect of p38 and MK2 kinase inhibitors on the inflammatory and toxicity biomarkers in vitro. Hum Exp Toxicol 37 521 PMID: 28629242
Haas et al (2013) The inflammatory kinase MAP4K4 promotes reactivation of Kaposi's sarcoma herpesvirus and enhances the invasiveness of infected endothelial cells. PLoS Pathog 9 e1003737 PMID: 24244164
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for VX 745
