Skip to main content

#161068

UCL-TRO-1938 PI3Ka activator

Cat. #161068

UCL-TRO-1938 PI3Ka activator

Cat. #: 161068

Unit size: 5mg

Availability: 3-4 weeks

Application: Signal transduction in a broad range of mammalian cells (human/rat/mouse)

£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. A small-molecule PI3Kα activator for cardioprotection and neuroregeneration. 2023. Nature. 618(7963):159-168. PMID: 37225977.

Tool Details
Handling
Target Details
Application Details
References

Tool Details

*FOR RESEARCH USE ONLY (for other uses, please contact the licensing team)

  • Tool name: UCL-TRO-1938 PI3Ka activator
  • Alternate name: 1938
  • Research fields: Cell signaling and signal transduction
  • Chemical name: 1-(7-((2-((4-(4-ethylpiperazin-1-yl)phenyl)amino )pyridin-4-yl)amino )indolin-1-yl)ethan- 1-one
  • Tool type ecom: Small Molecule
  • Primary target: PI3Kalpha - PIK3CA - phosphoinositide 3-kinase alpha - Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Alpha
  • Description: The PI3K signalling pathway plays a central role in tumour progression, and its inhibition has been a key focus for therapeutic applications and advances in cancer research. UCL-TRO-1938, specifically stimulates the activity of the PI3Kalpha isoform – an effector of growth factor signalling. 1938 selectively activates PI3Kalpha with minimal effects on other PI3Kalpha isoforms and kinases tested. 1938 allosterically activates PI3Kalpha through a mechanism distinct from physiological activators and induces transient activation of PI3Kalpha signalling in rodent and human cells.
  • Application: Signal transduction in a broad range of mammalian cells (human/rat/mouse)
  • 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 uM (see Gong et al. Nature). Do not use at concentrations above 10 uM 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: 5mg 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)

References

  • Gong GQ et al. A small-molecule PI3Kα activator for cardioprotection and neuroregeneration. 2023. Nature. 618(7963):159-168. PMID: 37225977
  • Kingwell K. PI3K activator taps route to regeneration. Nat Rev Drug Discov. 2023 Jul 22(7):537. PMID: 37291416.

Tool enquiry

Please ensure you use your organisation email address rather than personal where possible, as this helps us locate your organisation in our system faster.

Please note we may take up to three days to respond to your enquiry.

CancerTools.org uses the contact information provided to respond to you about our research tools and service. For more information please review our privacy policy.