理化性质和储存条件
| Molecular Weight (MW) | 467.02 |
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| Formula | C22H31ClN4O3S |
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| CAS No. | 1448189-80-7 (HCl salt) |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO:> 10 mM |
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| Water: > 50 mg/mL |
| Ethanol: N/A |
| Chemical Name | (2S,4R)-1-((S)-2-amino-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
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| Synonyms | Protein degrader 1 hydrochloride; Protein degrader 1 TFA;VH032-NH2 TFA; VHL ligand 1 TFA; Protein degrader 1 TFA , VHL-7526 TFA; VHL-7526; VHL7526; VHL 7526 |
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| SMILES Code | O=C([C@H](C[C@@H](O)C1)N1C([C@@H](N)C(C)(C)C)=O)NCC2=CC=C(C(SC=N3)=C3C)C=C2.Cl |
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实验参考方法
Protein degrader 1 HCl (hydrochloride) or PROTAC-VHL-ligand is a novel and potent small molecule ligand for VHL (Von Hippel-Lindau), which is an E3 ligase which has been targeted in many PROTAC (proteolysis-targeting chimeras) degraders. Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes. One method for inducing targeted protein degradation involves the use of PROTACs, heterobifunctional molecules that can recruit specific E3 ligases to a desired protein of interest. PROTACs have been successfully used to degrade numerous proteins in cells, but the peptidic E3 ligase ligands used in previous PROTACs have hindered their development into more mature chemical probes or therapeutics.
References: ACS Chem Biol. 2015 Aug 21;10(8):1831-7.
