PP 242

• Supplier: Tocris Bioscience
• Catalog: 1407
• Prices: $225.00, $925.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 1092351-67-1
• Chemical Name: 2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
• Formula: C16H16N6O
• Molecular Weight: 308.34
• Purity: >98 %
• Description: ATP-competitive mTORC1/mTORC2 inhibitor (IC 50 = 8 nM). Displays selectivity for mTOR over other PI 3K family kinases (IC 50 values are 0.102, 0.408, 1.27, 1.96 and 2.2 μ M for p110 γ , DNA-PK, p110 δ , p110 α and p110 β respectively) and 215 further kinases. Displays modest inhibition of PKC α , JAK2, PKC β I, PKC β II and RET (IC 50 values are 0.049, 0.110, 0.185, 0.198 and 0.224 μ M respectively). Inhibits both S6K and 4EBP1 phosphorylation; activity causes a decrease in cap-dependent protein translation. Also triggers downregulation of cFLIP S and augments TRAIL-induced apoptosis of cancer cells.

Product References

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and - Targeted polypharmacology: discovery of dual inhibitors of tyrosine and

Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA. Nat Chem Biol. 2008 Nov;4(11):691-9.

Effective and selective targeting of leukemia cells using a TORC1/2 kinase - Effective and selective targeting of leukemia cells using a TORC1/2 kinase

Janes MR, Limon JJ, So L, Chen J, Lim RJ, Chavez MA, Vu C, Lilly MB, Mallya S, Ong ST, Konopleva M, Martin MB, Ren P, Liu Y, Rommel C, Fruman DA. Nat Med. 2010 Feb;16(2):205-13.

mTOR complex 2 is involved in regulation of Cbl-dependent c-FLIP degradation and - mTOR complex 2 is involved in regulation of Cbl-dependent c-FLIP degradation and

Zhao L, Yue P, Khuri FR, Sun SY. Cancer Res. 2013 Mar 15;73(6):1946-57.