THS-044

• UNSPSC Description:

  THS-044 binding stabilizes the HIF2α PAS-B folded state, for regulating HIF2 activity in endogenous and clinical settings. Target: HIF2α Limited trypsin proteolysis reveals that both apo and THS-044-bound protein are efficiently cut at R330 in the extended HI loop. In the THS-044 bound state, there appears no additional proteolysis at the remaining candidate trypsin sites. In contrast, these THS-044-protected sites are protease accessible in the unliganded protein, leading its complete degradation. In parallel, NMR-based deuterium exchange measurements revealed a dramatic stabilization of the THS-044-bound protein β-sheet, with some sites experiencing 100-fold enhanced protection factors relative to the ligand-free protein.

• Target Antigen:

  HIF/HIF Prolyl-Hydroxylase

• Type:

  Reference compound

• Related Pathways:

  Metabolic Enzyme/Protease

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/THS-044.html

• Purity:

  99.67

• Solubility:

  DMSO : 125 mg/mL (ultrasonic)

• Smiles:

  FC(C1=CC=C(NN2CCOCC2)C([N+]([O-])=O)=C1)(F)F

• Molecular Weight:

  291.23

• References & Citations:

  [1]Motto I, et al. New aryl hydrocarbon receptor homology model targeted to improve docking reliability. J Chem Inf Model. 2011 Nov 28;51(11):2868-2881.|[2]Scheuermann TH, et al. Artificial ligand binding within the HIF2alpha PAS-B domain of the HIF2 transcription factor. Proc Natl Acad Sci U S A. 2009 Jan 13;106(2):450-455.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  No Development Reported

• CAS Number:

  62054-67-5