化学性质:
规格 | 10mM*1mLinDMSO 5mg 10mg 50mg |
CAS | 62054-67-5 |
别名 | N/A |
化学名 | N/A |
分子式 | C11H12F3N3O3 |
分子量 | 291.23 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
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.
[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.
特别提醒:
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标签:THS-044
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