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(S,R,S)-AHPC

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Chemical Structure| 1448297-52-6 同义名 : -
CAS号 : 1448297-52-6
货号 : A285256
分子式 : C22H30N4O3S
纯度 : 97%
分子量 : 430.564
MDL号 : MFCD29049827
存储条件:

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

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(243.87 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 25 mg/mL(58.06 mM)

动物实验配方:
生物活性
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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.61mL

2.32mL

1.16mL

23.23mL

4.65mL

2.32mL

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.