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Chemical Structure : UCL-TRO-1938
CAS No.: 2919575-27-0
Catalog No.: PC-20848Not For Human Use, Lab Use Only.
UCL-TRO-1938 (Compound 1938) is a selective, allosteric activator of PI3Kα with EC50 of 60 uM (based on in vitro lipid kinase activity), directly activates PI3Kα signalling in cells.
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|---|---|---|---|
| 5 mg | $228 | In stock | |
| 10 mg | $358 | In stock | |
| 25 mg | $558 | In stock | |
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| 100 mg | Get quote |
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UCL-TRO-1938 (Compound 1938) is a selective, allosteric activator of PI3Kα with EC50 of 60 uM (based on in vitro lipid kinase activity), directly activates PI3Kα signalling in cells.
UCL-TRO-1938 displays dissociation constant (Kd) values of 36 µM and 16 µM by rsurface plasmon resonance and differential scanning fluorimetry assays, respectively.
UCL-TRO-1938-stimulated PI3Kα activity is fully inhibited by the nanomolar potency ATP-competitive PI3Kα-selective inhibitor BYL719.
UCL-TRO-1938 does not affect the activity of the other PI3K isoforms in the panel (PI3Kβ, PI3Kγ, PI3Kδ, PI3K-C2α and VPS34) or the PI3K-related kinases PI4Kβ, mTOR and DNA-PK.
UCL-TRO-1938 stimulates PI3Kα by enhancing multiple events associated with natural and mutation-mediated PI3Kα activation. increases PtdIns(3,4,5)P3 levels in mouse embryonic fibroblasts (MEFs) with EC50 of 5 uM, increases pAKT(S473) levels in a concentration-dependent manner in MEFs with PI3Kα-WT with EC50 of 2-4 uM.
UCL-TRO-1938 dose-dependently increases metabolic activity in PI3Kα-WT but not in PI3Kα-KO MEFs with EC50 of 0.5 uM, induces cell cycle progression and an increase in cell numbe.
UCL-TRO-1938 demontrates cardioprotection effect and stimulates nerve regeneration in the rat sciatic nerve crush model of peripheral nerve injury and regeneration.
| M.Wt | 456.59 | |
| Formula | C27H32N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Ethanone, 1-[7-[[2-[[4-(4-ethyl-1-piperazinyl)phenyl]amino]-4-pyridinyl]amino]-2,3-dihydro-1H-indol-1-yl]- |
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1. Gong GQ, et al. Nature. 2023 May 24. doi: 10.1038/s41586-023-05972-2.
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