PP 242 | Tocris Bioscience 4257/5 product information

product summary

company name :

Tocris Bioscience

product type :

chemical

product name :

PP 242

catalog :

4257/5

quantity :

5 mg (also 25 mg)

price :

159 USD

more info or order :

Tocris Bioscience product webpage

citations: 10

Reference
Cioni J, Lin J, Holtermann A, Koppers M, Jakobs M, Azizi A, et al. Late Endosomes Act as mRNA Translation Platforms and Sustain Mitochondria in Axons. Cell. 2019;176:56-72.e15 pubmed publisher
Cagnetta R, Wong H, Frese C, Mallucci G, Krijgsveld J, Holt C. Noncanonical Modulation of the eIF2 Pathway Controls an Increase in Local Translation during Neural Wiring. Mol Cell. 2019;73:474-489.e5 pubmed publisher
Jacquin E, Leclerc Mercier S, Judon C, Blanchard E, Fraitag S, Florey O. Pharmacological modulators of autophagy activate a parallel noncanonical pathway driving unconventional LC3 lipidation. Autophagy. 2017;13:854-867 pubmed publisher
Holler C, Taylor G, McEachin Z, Deng Q, Watkins W, Hudson K, et al. Trehalose upregulates progranulin expression in human and mouse models of GRN haploinsufficiency: a novel therapeutic lead to treat frontotemporal dementia. Mol Neurodegener. 2016;11:46 pubmed publisher
Rodrik Outmezguine V, Okaniwa M, Yao Z, Novotny C, McWhirter C, Banaji A, et al. Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor. Nature. 2016;534:272-6 pubmed publisher
Ricoult S, Yecies J, Ben Sahra I, Manning B. Oncogenic PI3K and K-Ras stimulate de novo lipid synthesis through mTORC1 and SREBP. Oncogene. 2016;35:1250-60 pubmed publisher
Gao R, Zhao S, Jiang X, Sun Y, Zhao S, Gao J, et al. A large-scale screen reveals genes that mediate electrotaxis in Dictyostelium discoideum. Sci Signal. 2015;8:ra50 pubmed publisher
Thorne C, Wichaidit C, Coster A, Posner B, Wu L, Altschuler S. GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors. Nat Chem Biol. 2015;11:58-63 pubmed publisher
Fonseca B, Diering G, Bidinosti M, Dalal K, Alain T, Balgi A, et al. 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. 2012;287:17530-45 pubmed publisher
Ray R, Viar M, Johnson L. Amino acids regulate expression of antizyme-1 to modulate ornithine decarboxylase activity. J Biol Chem. 2012;287:3674-90 pubmed publisher

product information

brand :

Tocris

master code :

4257

SKU :

4257/5

rank :

0.0006

product name :

PP 242

description :

Dual mTORC1/mTORC2 inhibitor

target :

mTOR Inhibitors

category :

Small Molecules

sizes available :

5 mg (also 25 mg)

url print :

?utm_source=biocompare&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules

details of functionality :

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 M for p110 , DNA-PK, p110 , p110 and p110 respectively) and 215 further kinases. Displays modest inhibition of PKC , JAK2, PKC I, PKC II and RET (IC50 values are 0.049, 0.110, 0.185, 0.198 and 0.224 M 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.

extended description :

Dual mTORC1/mTORC2 inhibitor

chemical name text :

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

formula :

C 16 H 16 N 6 O

formula text :

C16H16N6O

cas num :

1092351-67-1

USD :

159 USD

product details :

Dual mTORC1/mTORC2 inhibitor

storage :

Store the unopened product at 2 - 8 °C. Do not use past expiration date.

more info or order :

Tocris Bioscience product webpage