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Submit ReviewPP 242
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% (HPLC)
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. PP 242 also inhibits oncogenic K-Ras and PI 3-K induced lipogenesis in breast cancer cells.
Compound Libraries for PP 242
PP 242 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for PP 242
| M. Wt | 308.34 |
| Formula | C16H16N6O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1092351-67-1 |
| PubChem ID | 25243800 |
| InChI Key | MTICIDWIKCANDD-WYMLVPIESA-N |
| Smiles | OC1=CC2=C(NC(C3=NN(C(C)C)C4=C3C(N)=NC=N4)=C2)C=C1 |
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 | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.71 | 25 |
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 |
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Product Datasheets for PP 242
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 PMID: 19209957
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
Ricoult et al (2016) Oncogenic PI3K and K-Ras stimulate de novo lipid synthesis through mTORC1 and SREBP. Oncogene 35 1250 PMID: 26028026
If you know of a relevant reference for PP 242, please let us know.
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Keywords: PP 242, PP 242 supplier, PP242, mtorc1/2, mtorc1, mtorc2, mammalian, target, rapamycin, dual, inhibitors, inhibits, selective, torkinib, cFLIPs, flice, like, inhibitory, protein, apoptosis, cancer, cells, mTOR, 4257, Tocris Bioscience
21 Citations for PP 242
Citations are publications that use Tocris products. Selected citations for PP 242 include:
Christian et al (2022) High-throughput translational profiling with riboPLATE-seq. Sci Rep 12 5718 PMID: 35383235
Elise et al (2022) V-ATPase is a universal regulator of LC3-associated phagocytosis and non-canonical autophagy. J Cell Biol 221 PMID: 35511089
Tatiana A et al (2022) Ribosomal leaky scanning through a translated uORF requires eIF4G2. Nucleic Acids Res 50 1111-1127 PMID: 35018467
Maria et al (2022) Inhibition of the SEC61 translocon by mycolactone induces a protective autophagic response controlled by EIF2S1-dependent translation that does not require ULK1 activity. Autophagy 18 841-859 PMID: 34424124
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
Sandra L et al (2023) Transcriptome, proteome, and protein synthesis within the intracellular cytomatrix. iScience 26 105965 PMID: 36824274
Paul C et al (2020) β1 integrin, ILK and mTOR regulate collagen synthesis in mechanically loaded tendon cells. Sci Rep 10 12644 PMID: 32724089
Adam et al (2020) Ribosome profiling reveals a functional role for autophagy in mRNA translational control. Commun Biol 3 388 PMID: 32681145
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
Thorne et al (2015) GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors. PLoS One 11 58 PMID: 25402767
Peng et al (2021) In vivo screen identifies a SIK inhibitor that induces β cell proliferation through a transient UPR. Nat Metab 3 682-700 PMID: 34031592
Anne et al (2021) Non-canonical autophagy drives alternative ATG8 conjugation to phosphatidylserine. Mol Cell 81 2031-2040.e8 PMID: 33909989
Selim et al (2021) Comparing mTOR inhibitor Rapamycin with Torin-2 within the RIST molecular-targeted regimen in neuroblastoma cells. Int J Med Sci 18 137-149 PMID: 33390782
Gao et al (2015) A large-scale screen reveals genes that mediate electrotaxis in Dictyostelium discoideum. Sci Signal 8 ra50 PMID: 26012633
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
Masaya et al (2019) NOX1-Dependent mTORC1 Activation via S100A9 Oxidation in Cancer Stem-like Cells Leads to Colon Cancer Progression. Cell Rep 28 1282-1295.e8 PMID: 31365870
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Cancer Metabolism Research Product Guide
This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
- Glycolysis
- Tricarboxylic Acid Cycle
- Lipidogenesis
- 1C Metabolism and Nucleic Acid Synthesis
- Drivers of Metabolic Reprogramming
- pH and Redox Balance
Cancer Metabolism Poster
This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.
Pathways for PP 242
