Chemical Name: 2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
Biological ActivityPP 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
mTOR complex 2 is involved in regulation of Cbl-dependent c-FLIP regulation and sensitivity of TRAIL-induced apoptosis.
Zhao et al.
Cancer Res., 2013;73:1946
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Apsel et al.
Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor.
Janes et al.
Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2.
Feldman et al.
PLoS Biol., 2009;7:371
Citations for PP 242
The citations listed below are publications that use Tocris products. Selected citations for PP 242 include:
10 Citations: Showing 1 - 10
Noncanonical Modulation of the eIF2 Pathway Controls an Increase in Local Translation during Neural Wiring.
Authors: Cagnetta Et al.
Mol Cell 2019;73:474
Late Endosomes Act as mRNA Translation Platforms and Sustain Mitochondria in Axons.
Authors: Cioni Et al.
Pharmacological modulators of autophagy activate a parallel noncanonical pathway driving unconventional LC3 lipidation.
Authors: Jacquin Et al.
Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor.
Authors: Rodrik-Outmezguine Et al.
Oncogenic PI3K and K-Ras stimulate de novo lipid synthesis through mTORC1 and SREBP.
Authors: Ricoult Et al.
Trehalose upregulates progranulin expression in human and mouse models of GRN haploinsufficiency: a novel therapeutic lead to treat frontotemporal dementia.
Authors: Holler Et al.
Mol Neurodegener 2016;11:46
A large-scale screen reveals genes that mediate electrotaxis in Dictyostelium discoideum.
Authors: Gao Et al.
Sci Signal 2015;8:ra50
GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors.
Authors: Thorne Et al.
PLoS One 2015;11:58
Amino acids regulate expression of antizyme-1 to modulate ornithine decarboxylase activity.
Authors: Ray Et al.
J Biol Chem 2012;287:3674
Structure-activity analysis of niclosamide reveals potential role for cytoplasmic pH in control of mammalian target of rapamycin complex 1 (mTORC1) signaling.
Authors: Fonseca Et al.
J Biol Chem 2012;287:17530
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