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Contributor Information

  • Name Bart Vanhaesebroeck
  • Institute University College London
  • Primary citation Gong GQ et al. 2023. Nature. 618(7963):159-168. PMID: 37225977.

Tool Details

  • Tool name: PI3Ka activator [UCL-TRO-1938™]
  • Alternate names: 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
  • Tool type: small molecule
  • Tool sub-type: kinase activator
  • Purpose: tool compound to probe for PI3Ka activity in cells and tissues
  • Molecular weight of the target: 456.59
  • Application: signal transduction in a broad range of mammalian cells (human/rat/mouse) - protection from cardiac ischaemia-reperfusion - neuroregeneration (in rats)
  • 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.
  • Research area: Cell signalling & Signal transduction
  • Selectivity: no activity on all other PI3K and PIKK isoforms tested - no relevant inhibition of kinases as determined by a kinase profiling screen (ThermoFischer).
  • 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.

  • For Research Use Only

Target Details

  • Target molecular weight: 456.59
  • 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)

Handling

  • Format: Dry
  • Purity: 99.65%
  • Solubility: Soluble in DMSO, Max conc. 10 mM
  • 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

Documentation

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References

  • •  Gong GQ et al. 2023. Nature. 618(7963):159-168. PMID: 37225977.