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  5. Tocris Bioscience™ PP 242

Tocris Bioscience™ PP 242
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Catalog No. 42575
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25 mg
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Catalog No. Quantity
42-575 5 mg
42-572-5 25 mg
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Catalog No. 42-575 Supplier Tocris Bioscience™ Supplier No. 4257/5
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Description

Dual mTORC1/mTORC2 inhibitor

PP 242 is an ATP-competitive mTORC1/mTORC2 inhibitor (IC50 = 8 nM). Displays selectivity for mTOR over other PI 3K family kinases (IC50 values are 0.102, 0.408, 1.27, 1.96 and 2.2 μM for p110γ, DNA-PK, p110δ, p110α and p110β respectively) and 215 further kinases. Displays modest inhibition of PKCα, JAK2, PKCβI, PKCβII and RET (IC50 values are 0.049, 0.110, 0.185, 0.198 and 0.224 μM respectively). Inhibits both S6K and 4EBP1 phosphorylation; activity causes a decrease in cap-dependent protein translation. Also triggers downregulation of cFLIPS and augments TRAIL-induced apoptosis of cancer cells. PP 242 also inhibits oncogenic K-Ras and PI 3-K induced lipogenesis in breast cancer cells.

Specifications

Chemical Name or Material 2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
CAS 1092351-67-1
Assay Percent Range >98%
Quantity 5 mg
Molecular Formula C16H16N6O
Formula Weight Observed MW: 308.34
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