Cat. #161068
PI3Ka activator [UCL-TRO-1938™]
Cat. #: 161068
Availability: Please enquire for quantities and pricing
Application: signal transduction in a broad range of mammalian cells (human/rat/mouse) - protection from cardiac ischaemia-reperfusion - neuroregeneration (in rats)
£250.00
This fee is applicable only for non-profit organisations. If you are a for-profit organisation or a researcher working on commercially-sponsored academic research, you will need to contact our licensing team for a commercial use license.
Contributor
Inventor: Bart Vanhaesebroeck
Institute: University College London
Primary Citation: Gong GQ et al. 2023. Nature. 618(7963):159-168. PMID: 37225977.
Tool Details
*FOR RESEARCH USE ONLY
- Tool name: PI3Ka activator [UCL-TRO-1938™]
- Alternate name: UCL-TRO-1938
- Molecular formula: C27H32N6O
- Chemical name: 1-(7-((2-((4-(4-ethylpiperazin-1-yl)phenyl)amino )pyridin-4-yl)amino )indolin-1-yl)ethan- 1-one
- Primary target: PI3Kalpha - PIK3CA - phosphoinositide 3-kinase alpha - Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Alpha
- Description: 1938 is a direct allosteric activator of PI3Kalpha, a key signalling molecule in cells. This tool allows to directly probe PI3Ka function in cells. PI3Ka is encoded by the PIK3CA gene, which is one of the most frequently mutated kinases in solid tumours. 1938 also activates both the wild-type and the oncogenic forms of PI3Kalpha.
- Application: signal transduction in a broad range of mammalian cells (human/rat/mouse) - protection from cardiac ischaemia-reperfusion - neuroregeneration (in rats)
- Purpose: tool compound to probe for PI3Ka activity in cells and tissues
- Selectivity: no activity on all other PI3K and PIKK isoforms tested - no relevant inhibition of kinases as determined by a kinase profiling screen (ThermoFischer).
- Molecular weight: 456.59
- Solubility: Soluble in DMSO, Max conc. 10 mM
- Additional notes: Use in cells at 1-10 microM (see Gong et al. Nature). Do not use at concentrations above 10 microM for cell-based assays longer than 24h.
Handling
- Format: Dry
- Purity: 0.9965
- Storage conditions: powder can be stored at room temperature - store aliquots of 10 mM stock dissoved in DMSO at -20C for shorter time (3 month) longer storage is recommended at -80C
- Shipping conditions: dry powder shipped at room temperature
Target Details
- Primary target: PI3Kalpha - PIK3CA - phosphoinositide 3-kinase alpha - Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Alpha
- Ec50 on primary target: 5 uM (based on PIP3 production as measured by PIP3 lipid production in cells by mass spectrometry); 2-4 uM (based on pAkt production in cells); 0.5 uM (based on ATP content in MEFs, using CellTiter-Glo, after 24h)
Application Details
- Application: signal transduction in a broad range of mammalian cells (human/rat/mouse) - protection from cardiac ischaemia-reperfusion - neuroregeneration (in rats)
References
- Gong GQ et al. 2023. Nature. 618(7963):159-168. PMID: 37225977.
