Millipore Sigma Vibrant Logo
Attention: We have moved. EMD Millipore products are no longer available for purchase on emdmillipore.com.Learn More

504379 HIF Inhibitor VII - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1422955-31-4C₁₂H₆ClFN₄O₃

Products

Catalog NumberPackaging Qty/Pack
5.04379.0001 Glass bottle 10 mg
Description
OverviewA 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.
Catalogue Number504379
Brand Family Calbiochem®
Synonyms0X3, N-(3-Chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine, Hypoxia-Inducible Factor Inhibitor VI
References
ReferencesWu, D., et al. 2015. Nature in press.
Scheuermann, T.H., et al. 2013. Nat. Chem. Biol. 9, 271.
Product Information
CAS number1422955-31-4
FormYellow powder
Hill FormulaC₁₂H₆ClFN₄O₃
Chemical formulaC₁₂H₆ClFN₄O₃
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetHIF-2α
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.04379.0001 04055977264067

Documentation

HIF Inhibitor VII - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Wu, D., et al. 2015. Nature in press.
Scheuermann, T.H., et al. 2013. Nat. Chem. Biol. 9, 271.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision12-February-2015 JSW
Synonyms0X3, N-(3-Chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine, Hypoxia-Inducible Factor Inhibitor VI
DescriptionA 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.
FormYellow powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1422955-31-4
Chemical formulaC₁₂H₆ClFN₄O₃
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (10 mg/ml). Use only fresh DMSO for reconstitution.
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesWu, D., et al. 2015. Nature in press.
Scheuermann, T.H., et al. 2013. Nat. Chem. Biol. 9, 271.