Catalog Number: 4257
Chemical Name: 2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
Biological Activity
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.
Technical Data
  • M.Wt:
    308.34
  • Formula:
    C16H16N6O
  • Solubility:
    Soluble to 25 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    1092351-67-1
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.
Background References
  1. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
    Apsel et al.
    Nat.Chem.Biol., 2008;4:691
  2. Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor.
    Janes et al.
    Nat.Med., 2010;16:205
  3. 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
  4. Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2.
    Feldman et al.
    PLoS Biol., 2009;7:371
Citations:

The citations listed below are publications that use Tocris products. Selected citations for PP 242 include:

4 Citations: Showing 1 - 4
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  1. A large-scale screen reveals genes that mediate electrotaxis in Dictyostelium discoideum.
    Authors: Gao Et al.
    Sci Signal 2015;8:ra50
  2. GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors.
    Authors: Thorne Et al.
    PLoS One 2015;11:58
  3. Amino acids regulate expression of antizyme-1 to modulate ornithine decarboxylase activity.
    Authors: Ray Et al.
    J Biol Chem 2012;287:3674
  4. 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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