PP 242

Pricing Availability   Qty
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)
Citations (10)
Literature (3)
Pathways (1)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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

10 Citations for PP 242

Citations are publications that use Tocris products. Selected citations for PP 242 include:

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

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

Do you know of a great paper that uses PP 242 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Pathways for PP 242

mTOR Signaling Pathway

mTOR Signaling Pathway

mTOR is a serine/threonine kinase that nucleates at multiprotein complexes mTORC1 and mTORC2. Signaling by these complexes regulates cell growth, proliferation and survival.