所有图片(1)
别名:
HIF Inhibitor VII, 0X3, Hypoxia-Inducible Factor Inhibitor VI, N-(3-Chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine, 0X3, N-(3-Chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine, Hypoxia-Inducible Factor Inhibitor VI, 504379
经验公式（希尔记法）:
C12H6ClFN4O3
推荐产品
检测方案
≥99% (HPLC)
质量水平
形式
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
yellow
溶解性
DMSO: 10 mg/mL
储存温度
2-8°C
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
一般描述
A cell-permeable benzoxadiazolamine that prevents HIF-2α-HIF-β/ARNT heterodimeration by perturbing HIF-2α Per-ARNT-Sim/PAS-B domain surface β-sheet conformation via a 1:1 stoichiometric binding (KD = 81 nM), while exhibiting no affinity toward HIF-1αPAS-B domain. Shown to be metabolically stable and non-cytotoxic in cultures and selectively inhibit hypoxia-induced HIF-2α DNA binding and HIF-2α-dependent EPO mRNA upregulation (1 to10 µM for 6 to 12 h), but not HIF-1α DNA binding or HIF-1α-dependent PGK1 mRNA upregulation, in Hep3B cells. Unlike HIF Inhibitors I-VI, this compound does not affect the cellular protein or mRNA levels of HIF-1α & HIF-2α.
A cell-permeable, metabolically stable (t1/2 = 14 h in 786-0 cultures; no metabolization up to 24 h in medium alone), non-cytotoxic (up to 30 µM & 24 h in 786-0 and Hep3B cultures) benzoxadiazolamine that prevents HIF-2α-HIF-β/ARNT (aryl hydrocarbon receptor nuclear translocator) heterodimeration by perturbing HIF-2α Per-ARNT-Sim/PAS-B domain surface β-sheet conformation via a 1:1 stoichiometric binding to HIF-2α PAS-B internal cavity (KD = 81 nM), while exhibiting no affinity toward HIF-1α PAS-B domain (KD >>5 µM). Shown to inhibit nuclear HIF-2α-ARNT, but not HIF-1α-ARNT, association in hypoxic Hep3B cells in a dose-dependent manner (0.1 to 10 µM) and selectively decrease hypoxia-induced HIF-2α DNA binding and HIF-2α-dependent EPO mRNA upregulation (% inhibition/time/dose = 60%/6 h/1 µM, 90%/6 h/10 µM, 45%/12 h/1 µM, 93%/12 h/10 µM), displaying little effect toward HIF-1α DNA binding or HIF-1α-dependent PGK1 mRNA upregulation. Unlike HIF Inhibitors I-VI, this compound does not affect the cellular protein or mRNA levels of HIF-1α & HIF-2α.
生化/生理作用
Cell permeable: yes
Primary Target
HIF-2α
HIF-2α
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Use only fresh DMSO for reconstitution.
其他说明
Wu, D., et al. 2015. Nature in press.
Scheuermann, T.H., et al. 2013. Nat. Chem. Biol.9, 271.
Scheuermann, T.H., et al. 2013. Nat. Chem. Biol.9, 271.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
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