UCL-TRO-1938 PI3Ka activator

UCL-TRO-1938 (1938) is a direct allosteric activator of PI3Kalpha, a key signalling molecule in cells. This tool allows direct probing of PI3Ka function in cells. PI3Ka is encoded by the PIK3CA gene, which is one of the most frequently mutated kinases in solid tumours. 1938 activates both the wild-type and the oncogenic forms of PI3Kalpha. […]

Contributors

Inventor Institute
Bart Vanhaesebroeck University College London
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.
Alternate name: 1938
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.
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).
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.

Images

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

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