UCL-TRO-1938 | PI3Kα activator | Probechem Biochemicals

Chemical Structure : UCL-TRO-1938

CAS No.: 2919575-27-0

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UCL-TRO-1938 (Compound 1938)

货号: 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.

规格	价格	库存
5 mg	￥1280	In stock
10 mg	￥1980	In stock
25 mg	￥3280	In stock
50 mg	￥5280	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	456.59
分子式	C27H32N6O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Ethanone, 1-[7-[[2-[[4-(4-ethyl-1-piperazinyl)phenyl]amino]-4-pyridinyl]amino]-2,3-dihydro-1H-indol-1-yl]-

参考文献

1. Gong GQ, et al. Nature. 2023 May 24. doi: 10.1038/s41586-023-05972-2.

UCL-TRO-1938 (Compound 1938)

生物&药学活性

物理化学性质&存储条件

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UCL-TRO-1938 (Compound 1938)

生物&药学活性

物理化学性质&存储条件

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