HIF-2α-IN-1

• CAT Number: I002339
• CAS Number: 1799948-06-3
• Molecular Formula: C16H8F5NO4S
• Molecular Weight: 405.295
• Purity: ≥95%
• Target: HIF-2α
• Solubility: 10 mM in DMSO
• Storage: -20°C
• IC50: ＜ 500 nM
• IUPAC Name: 3-[[(3R)-4-(difluoromethyl)-2,2-difluoro-3-hydroxy-1,1-dioxo-3H-1-benzothiophen-5-yl]oxy]-5-fluorobenzonitrile
• InChI: InChI=1S/C16H8F5NO4S/c17-8-3-7(6-22)4-9(5-8)26-10-1-2-11-13(12(10)15(18)19)14(23)16(20,21)27(11,24)25/h1-5,14-15,23H/t14-/m1/s1
• InChIKey: HZDKYXAZAPXCKQ-CQSZACIVSA-N
• SMILES: C1=CC2=C(C(C(S2(=O)=O)(F)F)O)C(=C1OC3=CC(=CC(=C3)C#N)F)C(F)F

HIF-2α-IN-1 (CAT: I002339) is a potent inhibitor of hypoxia-inducible factor-2α (HIF-2α). It exhibits an inhibitory effect on HIF-2α with an IC50 value of less than 500 nM in a HIF-2α scintillation proximity assay. HIF-2α is a transcription factor involved in cellular responses to hypoxia, playing a critical role in regulating genes associated with angiogenesis and tumor growth. By inhibiting HIF-2α, HIF-2α-IN-1 may disrupt the hypoxia signaling pathway and potentially have therapeutic implications in diseases such as cancer where HIF-2α is dysregulated. Further research is warranted to explore its therapeutic potential and selectivity.

Reference

[1]. Bruick Richard Keith, et al. HIF-2α inhibitors for treating iron overload disorders. From PCT Int. Appl. (2016), WO 2016057242 A1 20160414.
[2]. Dixon Darryl David, et al. Preparation of cyclic sulfone and sulfoximine analogs as HIF-2α inhibitors. From PCT Int. Appl. (2015), WO 2015095048 A1 20150625.