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重要文件

SML0883

Sigma-Aldrich

HIF-2 Antagonist 2

≥98% (HPLC)

同義詞:

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

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About This Item

經驗公式(希爾表示法):
C12H6ClFN4O3
CAS號碼:
分子量::
308.65
分類程式碼代碼:
12352200
NACRES:
NA.77
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品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 15 mg/mL, clear

儲存溫度

room temp

SMILES 字串

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 密鑰

CDQUJZKBRAFWNG-UHFFFAOYSA-N

生化/生理作用

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.

特點和優勢

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.

儲存類別代碼

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

水污染物質分類(WGK)

WGK 3


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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

文章

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.

我們提供各種小分子研究工具,例如轉錄因子調節劑、染色質修飾酵素的抑制劑,以及用於基因調控研究中靶點鑑定和驗證的激效劑/拮抗劑;以下是這些研究工具的精選。

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