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Submit ReviewVH 298
说明： High-affinity inhibitor of VHL
化学名： (2S,4R)-1-((S)-2-(1-cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
纯度： ≥98% (HPLC)
生物活性 for VH 298
VH 298 is a high-affinity inhibitor of E3 ubiquitin ligase VHL (Kd = 80-90 nM). Blocks interaction between VHL and HIF-α downstream of HIF-α hydroxylation, initiating hypoxic response. Results in time- and concentration-dependent accumulation of hydroxylated HIF-α, and upregulates mRNA and protein levels of HIF target genes, with similar transcriptional profile to hypoxia. Cell permeable.
Negative control cis VH 298 also available.
许可信息
Sold under licence from the University of Dundee
External Portal Information for VH 298
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of VH 298 is reviewed on the Chemical Probes website.
化合物库 for VH 298
VH 298 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for VH 298
| 分子量 | 523.65 |
| 公式 | C27H33N5O4S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2097381-85-4 |
| PubChem ID | 122199236 |
| InChI Key | NDVQUNZCNAMROD-RZUBCFFCSA-N |
| Smiles | O=C(N[C@@H](C(C)(C)C)C(N1C[C@@H](C[C@H]1C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)O)=O)C4(C#N)CC4 |
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 VH 298
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 52.37 | 100 | |
| ethanol | 52.37 | 100 |
制备储备液 for VH 298
以下数据基于产品分子量 523.65。 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 | 1.91 mL | 9.55 mL | 19.1 mL |
| 5 mM | 0.38 mL | 1.91 mL | 3.82 mL |
| 10 mM | 0.19 mL | 0.95 mL | 1.91 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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产品说明书 for VH 298
参考文献 for VH 298
参考文献是支持产品生物活性的出版物。
Frost et al (2015) Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat.Commun. 7 13312 PMID: 27811928
Soares et al (2018) Group-based optimization of potent and cell-active inhibitors of the von Hippel-Lindau (VHL) E3 ubiquitin ligase: structure-activity relationships leading to the chemical probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3. J.Med.Chem. 61 599 PMID: 28853884
Frost et al (2019) RNA-seq analysis of PHD and VHL inhibitors reveals differences and similarities to the hypoxia response. Wellcome Open Res. 4 17 PMID: 30801039
If you know of a relevant reference for VH 298, please let us know.
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关键词: VH 298, VH 298 supplier, Inhibitors, Inhibition, VH298, VHL, HIF-alpha, HIF-a, HIF-α, cisVH298, von, Hippel-Lindau, protein, E3, ubiquitin, ligase, Hypoxia, Inducible, Factors, Ubiquitin, Ligases, 6156, Tocris Bioscience
2 篇 VH 298 的引用文献
引用文献是使用了 Tocris 产品的出版物。 VH 298 的部分引用包括：
Qiu et al (2019) Von Hippel-Lindau (VHL) Protein Antagonist VH298 Improves Wound Healing in Streptozotocin-Induced Hyperglycaemic Rats by Activating Hypoxia-Inducible Factor- (HIF-) 1 Signalling. J Diabetes Res 2019 1897174 PMID: 30911550
Price et al (2019) Genome-Wide Interrogation of Human Cancers Identifies EGLN1 Dependency in Clear Cell Ovarian Cancers. Cancer Res 79 2564 PMID: 30898838
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