PP 242

Catalog # Availability Size / Price Qty
4257/25
4257/5
PP 242 | CAS No. 1092351-67-1 | mTOR Inhibitors
1 Image
Description: Dual mTORC1/mTORC2 inhibitor

Chemical Name: 2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol

Purity: ≥98%

Product Details
Citations (10)
Reviews

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. 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
  2. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
    Apsel et al.
    Nat.Chem.Biol., 2008;4:691
  3. Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor.
    Janes et al.
    Nat.Med., 2010;16:205
  4. Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2.
    Feldman et al.
    PLoS Biol., 2009;7:371

Product Datasheets

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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

  1. Noncanonical Modulation of the eIF2 Pathway Controls an Increase in Local Translation during Neural Wiring.
    Authors: Cagnetta Et al.
    Mol Cell  2019;73:474
  2. Late Endosomes Act as mRNA Translation Platforms and Sustain Mitochondria in Axons.
    Authors: Cioni Et al.
    Cell  2019;176:56
  3. Pharmacological modulators of autophagy activate a parallel noncanonical pathway driving unconventional LC3 lipidation.
    Authors: Jacquin Et al.
    Autophagy  2017;13:854
  4. Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor.
    Authors: Rodrik-Outmezguine Et al.
    Nature  2016;534:272
  5. Oncogenic PI3K and K-Ras stimulate de novo lipid synthesis through mTORC1 and SREBP.
    Authors: Ricoult Et al.
    Oncogene  2016;35:1250
  6. 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
  7. A large-scale screen reveals genes that mediate electrotaxis in Dictyostelium discoideum.
    Authors: Gao Et al.
    Sci Signal  2015;8:ra50
  8. GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors.
    Authors: Thorne Et al.
    PLoS One  2015;11:58
  9. Amino acids regulate expression of antizyme-1 to modulate ornithine decarboxylase activity.
    Authors: Ray Et al.
    J Biol Chem  2012;287:3674
  10. 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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