UCL-TRO-1938 PI3Ka activator

Contributors

Inventor Institute
Bart Vanhaesebroeck University College London
SKU: 161068
Product 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.
Alternate name: 1938
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.
Molecular weight: 456.59
Chemical name: 1-(7-((2-((4-(4-ethylpiperazin-1-yl)phenyl)amino )pyridin-4-yl)amino )indolin-1-yl)ethan- 1-one
Selectivity: No activity on all other PI3K and PIKK isoforms tested – no relevant inhibition of kinases as determined by a kinase profiling screen (ThermoFischer).
Cat. #: 161068
Unit size: 5mg
Research Fields: Cell signaling and signal transduction
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
Primary citation: Gong GQ et al. A small-molecule PI3Kα activator for cardioprotection and neuroregeneration. 2023. Nature. 618(7963):159-168. PMID: 37225977.
Primary target: PI3Kalpha – PIK3CA – phosphoinositide 3-kinase alpha – Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Alpha
Format: Dry
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
Solubility: Soluble in DMSO, Max conc. 10 mM
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.

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Chemical structure
Graph plotting the activation of PI3K isoforms using 1938 a PI3Kalpha activator

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