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Pp242 (TORKinib) mTOR Inhibitor

Catalog # CD0258

Price:  1 mg - $15; 5 mg - $29; 10 mg - $37; 25 mg - $73; 50 mg - $133; 100 mg - $245; 250 mg - $546; 500 mg - $919; 1 g $1800

Availability:  In stock

 

 

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

 

White to off white solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Purity: 99% by HPLC. CAS# 1092351-67-1. Solubility: DMSO (10 mg/mL), DMF (20 mg/mL); DMF : PBS 1 : 1 (0.5 mg/mL). Molecular Formula: C16H16N6O. Molecular Weight: 308.3.

 

 

 

A cell-permeable pyrazolopyrimidine compound that acts as a potent, reversible, and ATP-competitive inhibitor against both mTORC1 & mTORC2 (IC50 = 30 & 58 nM, respectively, with 100 M ATP). PP242 inhibits PKCα, p110γ, and JAK2 with 6-, 13-, and 14-fold less potency and exhibits much reduced or no activity against a panel of 216 other kinases at a concentration of 1 M (maximum of 68% or 77% inhibition observed with 10 or 100 M ATP, respectively). PP242 differentially inhibits insulin-stimulated phosphorylations of cellular proteins both in cultures (2.5 M) in vitro and in mice (20 mg/kg i.p.) in vivo in a manner distinctly different from that seen in mTORC2-functional knockout SIN1-/- cells or in cultures treated with Rapamycin, which targets only mTORC1, but not mTORC2. Blockage of 4EBP1 T36/T45/S65 phosphorylation by PP242 upon insulin stimulation in primary MEFs correlates well with an enhanced 4EBP1 association with the cap-binding protein eIF4E, resulting in a selective inhibition of cap-dependent, but not cap-independent, protein translation.

 

 

References: 1. Apsel, B. et al. Nat. Chem. Biol. 2008, 4, 691; 2. Feldman, F. E. et al. PLoS Biology 2009, 7, 371; 3. Hsieh, A. C. et al Cancer Cell 2010, 17, 241.

 

 

SAME PRODUCT AS:

Axxora 

Cat. No. BV-1658

 

Cayman Chemical  

Cat. No. 13643

Enzo Life Sciences 

Cat. No. N/A

EMD

Cat. No. 475988

Tocris   

Cat. No. 4257

Sigma

Cat. No. P037

 

 

Caution Not fully tested. For research use only. Not for human use.

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