Cat. No. 4257
Chemical Name: 2-[4-Amino-1-(1-methylethyl)-1H-pyr
Biological ActivityATP-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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
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.
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.
Apsel et al (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat.Chem.Biol. 4 691. PMID: 18849971.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products. Selected citations for PP 242 include:
Gao et al (2015) A large-scale screen reveals genes that mediate electrotaxis in Dictyostelium discoideum. Sci Signal 8 ra50. PMID: 26012633.
Thorne et al (2015) GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors. PLoS One 11 58. PMID: 25402767.
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.
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Keywords: PP 242, supplier, PP242, mtorc1/2, mtorc1, mtorc2, mammalian, target, rapamycin, dual, inhibitors, inhibits, selective, torkinib, cFLIPs, flice, like, inhibitory, protein, apoptosis, cancer, cells, Tocris Bioscience, mTOR Inhibitor products
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