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.
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
HIF-1α
Reversible: yes
Secondary Target
VEGF
Target IC50: 14 nM in HRE-Luc HeLa cells
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
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
Molecular Weight: 305.33. Empirical Formula: C18H15N3O2. Assay: ≥. 98% (HPLC). Quality Level: 100. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 41115701
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5382540001