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CAS No.: 1448297-52-6

(2S,4R)-1-((S)-2-Amino-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide Catalog No. CSN20357

Synonyms: VH032-NH2;VHL ligand 1;VHL Ligand for PROTAC

MDK7526 is a ligand of Von Hippel–Lindau protein, that can be used for making proteolysis targeting chimeras (PROTACs).

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技术信息

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描述Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Small-molecule-based proteolysis targeting chimeras (PROTACs) have been developed to degrade targeted proteins. The von Hippel–Lindau (VHL) is a component of a multi-subunit E3 ubiquitin ligase that functions with a cullin RING ligase under normoxic conditions to degrade HIF1a^[3]. MDK7526 is a ligand of Von Hippel–Lindau protein that can be used for making PROTACs.
作用机制MDK7526 contains an isoxazolylacetamide fragment, which was designed to interact with a water molecule previously identified as an important part of the hydrogen-bonding network between VHL and HIF1a.
参考文献

[1] Bondeson DP, Crews CM. Targeted Protein Degradation by Small Molecules. Annu Rev Pharmacol Toxicol. 2017 Jan 6;57:107-123.
[2] Bondeson DP, Mares A, et al. Catalytic in vivo protein knockdown by small-molecule PROTACs. Nat Chem Biol. 2015 Aug;11(8):611-7.
[3] Buckley DL, Gustafson JL, Van Molle I, Roth AG, Tae HS, Gareiss PC, Jorgensen WL, Ciulli A, Crews CM. Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α. Angew Chem Int Ed Engl. 2012 Nov 12;51(46):11463-7. doi: 10.1002/anie.201206231. Epub 2012 Oct 12. PMID: 23065727; PMCID: PMC3519281.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3225 mL
- 11.6127 mL
- 23.2254 mL
- 5 mM
- 0.4645 mL
- 2.3225 mL
- 4.6451 mL
- 10 mM
- 0.2323 mL
- 1.1613 mL
- 2.3225 mL

技术信息

CAS号

1448297-52-6

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H30N4O3S

运输

蓝冰

分子量

430.56

别名

VH032-NH2;VHL ligand 1;VHL Ligand for PROTAC;Protein Degrader 1;MDK-7526;ULM-1;VH032 desacetyl;VH032 amine;Degradation Inducing Moiety A

溶解度

DMSO	105.0 mg/mL (243.9 mM)
Water	insoluble

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(2S,4R)-1-((S)-2-Amino-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide Catalog No. CSN20357

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