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SML0883

HIF-2 Antagonist 2

≥98% (HPLC)

Synonym(s):

N-(3-Chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine, TC-S7009

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About This Item

Empirical Formula (Hill Notation):
C12H6ClFN4O3
CAS Number:
1422955-31-4
Molecular Weight:
308.65
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
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Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 15 mg/mL, clear

storage temp.

room temp

SMILES string

Fc1cc(cc(c1)Nc2c(c3n[o]nc3cc2)[N+](=O)[O-])Cl

InChI

1S/C12H6ClFN4O3/c13-6-3-7(14)5-8(4-6)15-10-2-1-9-11(17-21-16-9)12(10)18(19)20/h1-5,15H

InChI key

CDQUJZKBRAFWNG-UHFFFAOYSA-N

Biochem/physiol Actions

HIF-2α antagonist.
Hypoxia inducible transcription factors (HIF) control gene expression when oxygen availability is low and are associated with the onset and progression of a variety of cancers. They are heterodimers of an HIF-α (HIF-1α, HIF-2α also known as EPAS-1, or HIF-3α) and aryl hydrocarbon receptor nuclear translocator (ARNT, also known as HIF-β). N-(3-Chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine is a highly selective antagonist of HIF-2 heterodimerization, DNA-binding activity, and target gene transcription. It binds the HIF-2α PAS-B domain with a KD ~80 nM compared to a KD > 5000 nM for the HIF-1α PAS-B domain.

Features and Benefits

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

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Certificates of Analysis (COA)

Lot/Batch Number
0000438627
0000438627
0000247051
0000247051
0000132631

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Isabelle Westerlund et al.
Biochemical and biophysical research communications, 508(4), 1233-1239 (2018-12-20)
The hypoxia inducible transcription factor EPAS1/HIF2α has been described as an oncogene and a potential therapeutic target in neuroblastoma. Our analysis of several neuroblastoma tumour expression datasets does not support an oncogenic role, instead EPAS1 expression is associated with better
Kyoko Endo et al.
International journal of molecular sciences, 21(1) (2019-12-22)
Previous studies have reported the up-regulation of the two-pore domain K+ channel K2P5.1 in the CD4+ T cells of patients with multiple sclerosis (MS) and rheumatoid arthritis (RA), as well as in a mouse model of inflammatory bowel disease (IBD).
Bo Zhang et al.
Cells, 11(16) (2022-08-27)
Hypoxia-inducible factor (HIF) directly activates the transcription of metabolic enzymes in response to hypoxia to reprogram cellular metabolism required for tumor cell proliferation. Through analyzing glutamate-linked aminotransferases, we here identified glutamate pyruvate transaminase 2 (GPT2) as a direct HIF-2 target
Fumihito Hikage et al.
Endocrinology, 160(1), 20-35 (2018-11-06)
Thyroid-associated orbitopathy (TAO) is a disfiguring periocular connective tissue disease associated with autoimmune thyroid disorders. It is a potentially blinding condition, for which no effective pharmacological treatment has been established. Despite a suggested role played by autoimmune thyrotropin receptor activation

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Discover Bioactive Small Molecules for Gene Regulation

We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

Global Trade Item Number

SKUGTIN
SML0883-25MG04061832824956
SML0883-5MG04061832824963

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