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Biological Activity for PP 242
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.
Compound Libraries for PP 242
Technical Data for PP 242
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PP 242
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for PP 242
The following data is based on the product molecular weight 308.34. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.25 mM||12.97 mL||64.86 mL||129.73 mL|
|1.25 mM||2.59 mL||12.97 mL||25.95 mL|
|2.5 mM||1.3 mL||6.49 mL||12.97 mL|
|12.5 mM||0.26 mL||1.3 mL||2.59 mL|
References for PP 242
References are publications that support the biological activity of the product.
Apsel et al (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat.Chem.Biol. 4 691 PMID: 18849971
Janes et al (2010) Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nat.Med. 16 205 PMID: 20072130
Feldman et al (2009) Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol. 7 371
Zhao et al (2013) mTOR complex 2 is involved in regulation of Cbl-dependent c-FLIP regulation and sensitivity of TRAIL-induced apoptosis. Cancer Res. 73 1946 PMID: 23319802
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10 Citations for PP 242
Citations are publications that use Tocris products. Selected citations for PP 242 include:
Jacquin et al (2017) Pharmacological modulators of autophagy activate a parallel noncanonical pathway driving unconventional LC3 lipidation. Autophagy 13 854 PMID: 28296541
Rodrik-Outmezguine et al (2016) Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor. Nature 534 272 PMID: 27279227
Holler et al (2016) Trehalose upregulates progranulin expression in human and mouse models of GRN haploinsufficiency: a novel therapeutic lead to treat frontotemporal dementia. Mol Neurodegener 11 46 PMID: 27341800
Thorne et al (2015) GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors. PLoS One 11 58 PMID: 25402767
Cioni et al (2019) Late Endosomes Act as mRNA Translation Platforms and Sustain Mitochondria in Axons. Cell 176 56 PMID: 30612743
Cagnetta et al (2019) Noncanonical Modulation of the eIF2 Pathway Controls an Increase in Local Translation during Neural Wiring. Mol Cell 73 474 PMID: 30595434
Gao et al (2015) A large-scale screen reveals genes that mediate electrotaxis in Dictyostelium discoideum. Sci Signal 8 ra50 PMID: 26012633
Ricoult et al (2016) Oncogenic PI3K and K-Ras stimulate de novo lipid synthesis through mTORC1 and SREBP. Oncogene 35 1250 PMID: 26028026
Fonseca et al (2012) Structure-activity analysis of niclosamide reveals potential role for cytoplasmic pH in control of mammalian target of rapamycin complex 1 (mTORC1) signaling. J Biol Chem 287 17530 PMID: 22474287
Ray et al (2012) Amino acids regulate expression of antizyme-1 to modulate ornithine decarboxylase activity. J Biol Chem 287 3674 PMID: 22157018
Do you know of a great paper that uses PP 242 from Tocris? Please let us know.
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Literature in this Area
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