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PC1007 VH 032, Amine Hydrochloride 5mg

$35.00
  • Product Code: PC1007 VH 032, Amine Hydrochloride 5mg
  • Availability: Contact us for lead time
Tags: PROTAC

Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes. Protein degraders have the power to abrogate all of the functions of a drug target at once, including scaffolding functions which are difficult to target with small molecule inhibitors. A novel class of PROTACs that incorporate small molecule VHL ligands to successfully degrade HaloTag7 fusion proteins is developed. HaloPROTACs will inspire the development of future PROTACs with more drug-like properties. In HEK 293 cells stably expressing GFP-HaloTag7, 24 hour treatment with HaloPROTAC1 leads to less than 20% degradation, the longer HaloPROTAC2 leads to nearly 70% degradation of GFP-Halotag7 at 2.5 μM. HaloPROTACs containing protein degrader 1 leads to nearly 70% degradation of GFP-HaloTag7, when sufficiently long linkers are used. Derivative of the von Hippel-Lindau (VHL) ligand, VH 032, commonly used as a precursor to PROTACs that hijack VHL as the E3 ubiquitin ligase component. Supplied with a primary amine functional handle at a position known not to significantly affect binding to VHL, for ready conjugation to a linker/target protein ligand.


Application:


Functionalized VHL ligand for PROTACs


Product Information:


Purity:                                  >98% 

MW:                                    467.02

Formula:                                  C22H31ClN4O3S

CAS No.                                  1448189-80-7

Physical State:                 Lyophilized white powder

Quantity:                                 5 mg; 10 mg; 25 mg

Solubility:                                 40 mg/mL in DMSO

Storage:                                 Store desiccated as supplied at -20°C for up to 3 years. Store solutions at -80°C for up to 6 months or -20°C for up to 1 month.


Documents



References


1.    Buckley DL et al. HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins. ACS Chem Biol. 2015 Aug 21;10(8):1831-7.

2.    Zengerle et al (2015) Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS Chem.Biol. 10 1770 PMID: 26035625

3.    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 




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