5.38254

GN44028

• 别名: GN44028, N -(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine, HIF-1 Inhibitor II
• 经验公式（希尔记法）: C₁₈H₁₅N₃O₂
• 分子量: 305.33
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 化驗: ≥98% (HPLC)
• 品質等級: 100
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: brown
• 溶解度: DMSO: 50 mg/mL
• 儲存溫度: 2-8°C

说明

一般說明

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.

生化／生理作用

Cell permeable: yes

Primary Target
HIF-1α

Reversible: yes

Secondary Target
VEGF

Target IC₅₀: 14 nM in HRE-Luc HeLa cells

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他說明

Minegishi, H., et al. 2013. ACS Med. Chem. Lett.4, 297.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable