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HIF-2α-IN-3

Names

[ CAS No. ]:
313964-19-1

[ Name ]:
HIF-2α-IN-3

Biological Activity

[Description]:

HIF-2α-IN-3, an allosteric inhibitor of hypoxia inducible factor-2α (HIF-2α), exhibits an IC50 of 0.4 µM and a KD of 1.1 µM. Anticancer agent[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase

[Target]

IC50: 0.4 µM (HIF-2α)[1] KD: 1.1 µM (HIF-2α)[1]


[In Vitro]

HIF-2α-IN-3 (Compound 1) inhibit HIF-2α-ARNT (also known as HIF-β) heterodimerization by binding an internal cavity of the HIF-2α PAS-B domain[1].

[References]

[1]. Rogers JL, et al. Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor. J Med Chem. 2013 Feb 28;56(4):1739-47.

Chemical & Physical Properties

[ Molecular Formula ]:
C12H6ClN5O5

[ Molecular Weight ]:
335.66

[ Storage condition ]:
2-8°C

Related Compounds