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Submit ReviewVH 032
说明： Inhibitor of VHL; blocks interaction of VHL and HIF-α
化学名： (2S,4R)-1-((S)-2-Acetamido-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 032
VH 032 is an inhibitor of E3 ubiquitin ligase VHL (Kd = 185 nM). Blocks interaction between VHL and HIF-α downstream of HIF-α hydroxylation, initiating hypoxic response. VH 032 treatment causes dose dependent upregulation of HIF-target genes including CA9, GLUT1 and PHD2 in different cell lines. Cell permeable.
技术数据 for VH 032
| 分子量 | 472.6 |
| 公式 | C24H32N4O4S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1448188-62-2 |
| PubChem ID | 77232228 |
| InChI Key | GFVIEZBZIUKYOG-SVFBPWRDSA-N |
| Smiles | CC(N[C@@H](C(C)(C)C)C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O |
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 032
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 47.26 | 100 | |
| ethanol | 47.26 | 100 |
制备储备液 for VH 032
以下数据基于产品分子量 472.6。 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 | 2.12 mL | 10.58 mL | 21.16 mL |
| 5 mM | 0.42 mL | 2.12 mL | 4.23 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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产品说明书 for VH 032
参考文献 for VH 032
参考文献是支持产品生物活性的出版物。
Galdeano et al (2014) Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von Hippel-Lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities. J.Med.Chem. 57 8657 PMID: 25166285
Frost et al (2016) Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat.Commun. 7 13312 PMID: 27811928
If you know of a relevant reference for VH 032, please let us know.
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关键词: VH 032, VH 032 supplier, VH032, Inhibitors, Inhibition, inhibits, VHL, HIF-alpha, HIF-a, HIF-α, von, Hippel-Lindau, protein, E3, ubiquitin, ligase, Hypoxia, Inducible, Factors, Ubiquitin, Ligases, 7774, Tocris Bioscience
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