Product Description: THS-044 binding stabilizes the HIF2α PAS-B folded state, for regulating HIF2 activity in endogenous and clinical settings.Target: HIF2αLimited 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.
Applications: Cancer-programmed cell death
Formula: C11H12F3N3O3
References: [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.
CAS Number: 62054-67-5
Molecular Weight: 291.23
Compound Purity: 99.67
Research Area: Cancer
Solubility: DMSO : 125 mg/mL (ultrasonic)
Target: HIF/HIF Prolyl-Hydroxylase
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