5.38254
GN44028
Synonym(s):
GN44028, N -(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine, HIF-1 Inhibitor II
Sign In to View Organizational & Contract Pricing.
Select a Size
Change View
About This Item
Empirical Formula (Hill Notation):
C18H15N3O2
Molecular Weight:
305.33
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
Quality Segment
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
brown
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
A cell-permeable indenopyrazole based compound that potently suppresses hypoxia-induced HIF-1α transcription (IC50 = 14 nM in HRE-Luc HeLa cells) and VEGF-expression. Shown to effectively induce growth arrest in several cancer cells (IC50 = 2.1, 3.7 & 1.8 µM for HCT116, HepG2 & HeLa cells), although with reduced efficiency in PC3 (IC50 = 25.4 µM). Does neither affect HIF-1α protein accumulation nor HIF-1α/HIF-1β heterodimer complex formation. Suggested to act via impairing HIF-1α/HIF-1β heterodimer-induced transcriptional pathway.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
HIF-1α
HIF-1α
Reversible: yes
Secondary Target
VEGF
VEGF
Target IC50: 14 nM in HRE-Luc HeLa cells
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Minegishi, H., et al. 2013. ACS Med. Chem. Lett.4, 297.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.