THS-044

THS-044 is a modulator of the formation of the HIF2α/ARNT heterodimer. THS-044 binding stabilizes the HIF2α PAS-B folded state (KD = 2 μM), for regulating HIF2 activity in endogenous and pathological settings, and does not bind to HIF1α or ARNT PAS-B. THS-044 increases the KD of the heterodimer formed by HIF2α PAS-B and ARNT PAS-B from 120 μM to 400 μM. THS-044 can be used for the study of diseases related to hypoxia[1][2].

Product Specifications

CAS Number

62054-67-5

UNSPSC

12352005

Target

HIF/HIF Prolyl-Hydroxylase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/THS-044.html

Purity

99.67

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

FC(C1=CC=C(NN2CCOCC2)C([N+]([O-])=O)=C1)(F)F

Molecular Formula

C11H12F3N3O3

Molecular Weight

291.23

References & Citations

[1]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.|[2]Nordgren, Ida Karin, and Ali Tavassoli. Targeting tumour angiogenesis with small molecule inhibitors of hypoxia inducible factor. Chemical Society Reviews 40.8 (2011) : 4307-4317.