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| Product Name: | VH298 | | Synonyms: | VH298;VH298;VH 298;CS-2647;(2S,4R)-1-((S)-2-(1-cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;VH298 USP/EP/BP;(2S,4R)-1-[(2S)-2-[(1-cyanocyclopropanecarbonyl)amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide;(2S,4R)-1-((S)-2-(1-Cyanocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide | | CAS: | 2097381-85-4 | | MF: | C27H33N5O4S | | MW: | 523.65 | | EINECS: | | Product Categories: | | Mol File: | 2097381-85-4.mol |
| VH298 Chemical Properties |
| Boiling point | 860.8±65.0 °C(Predicted) | | density | 1.33±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | pka | 12.28±0.20(Predicted) |
| VH298 Usage And Synthesis |
| Description | VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. VH298 blocks the VHL:HIF-α interaction with Kd of 90 nM in isothermal titration calorimetry (ITC) and 80 nM in a competitive fluorescence polarization assay. VH-298 can be used in PROTAC technology. | | In vitro | VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. VH298 promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. VH298 improves the angiogenesis of hUVEC. | | In vivo | VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. VH298 promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. VH298 improves the angiogenesis of hUVEC. | | Description | VH-298 is a E3 ligase ligand-linker conjugate that couples the VHL ligand and blocks the interaction between VHL and HIF-α, initiating hypoxic response. | | Uses | (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide is a VHL inhibitors that decreases hypoxia inducible factor-α during hypoxia associated signaling in human cervical cancer, osteosarcoma HeLa and U2OS. cells. |
| VH298 Preparation Products And Raw materials |
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