TC-S 7009 是一种有效的选择性 HIF-2α 抑制剂，Kd 为 81 nM。
货号:ajcx26976
CAS:1422955-31-4
分子式:C12H6ClFN4O3
分子量：308.65
溶解度:DMSO: 30 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

High affinity and selective HIF-2α inhibitor (Kd = 81 nM). Binds to the HIF-2α PAS-B domain; disrupts HIF-2α-ARNT heterodimerization. Exhibits >60-fold selectivity for HIF-2α over HIF-1α. Decreases HIF-2α DNA-binding and attenuates expression of HIF-2α target genes in vitro.

Scheuermann et al (2013) Allosteric inhibition of hypoxia inducible factor-2 with small molecules. Nat.Chem.Biol. 9 271 PMID:23434853 |Rogers et al (2013) Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor. J.Med.Chem. 56 1739 PMID:23363003 |Wu et al (2019) Bidirectional modulation of HIF-2 activity through chemical ligands. Nat.Chem.Biol. 15 367 PMID:30804532