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PP 242

Catalog #: 4257
21 Citations Datasheet
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 (21)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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. PP 242 also inhibits oncogenic K-Ras and PI 3-K induced lipogenesis in breast 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.

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Citations for PP 242

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

21 Citations: Showing 1 - 10

  1. Transcriptome, proteome, and protein synthesis within the intracellular cytomatrix.
    Authors: Sandra L Et al.
    iScience  2023;26:105965
  2. Ribosomal leaky scanning through a translated uORF requires eIF4G2.
    Authors: Tatiana A Et al.
    Nucleic Acids Res  2022;50:1111-1127
  3. V-ATPase is a universal regulator of LC3-associated phagocytosis and non-canonical autophagy.
    Authors: Elise Et al.
    J Cell Biol  2022;221
  4. Inhibition of the SEC61 translocon by mycolactone induces a protective autophagic response controlled by EIF2S1-dependent translation that does not require ULK1 activity.
    Authors: Maria Et al.
    Autophagy  2022;18:841-859
  5. High-throughput translational profiling with riboPLATE-seq.
    Authors: Christian Et al.
    Sci Rep  2022;12:5718
  6. Non-canonical autophagy drives alternative ATG8 conjugation to phosphatidylserine.
    Authors: Anne Et al.
    Mol Cell  2021;81:2031-2040.e8
  7. In vivo screen identifies a SIK inhibitor that induces β cell proliferation through a transient UPR.
    Authors: Peng Et al.
    Nat Metab  2021;3:682-700
  8. Comparing mTOR inhibitor Rapamycin with Torin-2 within the RIST molecular-targeted regimen in neuroblastoma cells.
    Authors: Selim Et al.
    Int J Med Sci  2021;18:137-149
  9. Ribosome profiling reveals a functional role for autophagy in mRNA translational control.
    Authors: Adam Et al.
    Commun Biol  2020;3:388
  10. β1 integrin, ILK and mTOR regulate collagen synthesis in mechanically loaded tendon cells.
    Authors: Paul C Et al.
    Sci Rep  2020;10:12644
  11. Noncanonical Modulation of the eIF2 Pathway Controls an Increase in Local Translation during Neural Wiring.
    Authors: Cagnetta Et al.
    Mol Cell  2019;73:474
  12. NOX1-Dependent mTORC1 Activation via S100A9 Oxidation in Cancer Stem-like Cells Leads to Colon Cancer Progression.
    Authors: Masaya Et al.
    Cell Rep  2019;28:1282-1295.e8
  13. Late Endosomes Act as mRNA Translation Platforms and Sustain Mitochondria in Axons.
    Authors: Cioni Et al.
    Cell  2019;176:56
  14. Pharmacological modulators of autophagy activate a parallel noncanonical pathway driving unconventional LC3 lipidation.
    Authors: Jacquin Et al.
    Autophagy  2017;13:854
  15. Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor.
    Authors: Rodrik-Outmezguine Et al.
    Nature  2016;534:272
  16. Oncogenic PI3K and K-Ras stimulate de novo lipid synthesis through mTORC1 and SREBP.
    Authors: Ricoult Et al.
    Oncogene  2016;35:1250
  17. 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
  18. A large-scale screen reveals genes that mediate electrotaxis in Dictyostelium discoideum.
    Authors: Gao Et al.
    Sci Signal  2015;8:ra50
  19. GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors.
    Authors: Thorne Et al.
    PLoS One  2015;11:58
  20. Amino acids regulate expression of antizyme-1 to modulate ornithine decarboxylase activity.
    Authors: Ray Et al.
    J Biol Chem  2012;287:3674
  21. 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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