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PP242 | mTOR inhibitor

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Price:
$89.00
Catalog #:
C7724-5
Quantity:


Product Description

PP242 is an ATP-competitive, pyrazolopyrimidine-based inhibitor of mTOR at an IC50 of 8 nM. It is highly selective against the PI3K family of kinases, with all but one isoform (p110g IC50 = 102 nM) registering with IC50s > 1 uM. In a broad kinase panel, PP242 showed modest activity only in PKCa and JAK2 at IC50s of 49 and 110 nM, respectively. [1] PP242 inhibits insulin-stimulated phosphorylation of Akt at S473, as well as phosphorylation at T308.

PP242 inhibits TORC1 and TORC2 function and inhibits phosphorylation (S473) in studies where Rapamycin has been shown to be less effective. Moreover, phosphorylation studies on S2481, a marker for TORC2 activity, showed that PP242 inhibition was significant, whereas rapamycin had little effect. [2] Cell-cycle analysis showed that PP242 induced both arrest and apoptosis, whereas rapamycin was cytostatic. [3]


Technical information:

Chemical Formula:   C16H16N6O
CAS #:   1092351-67-1
Molecular Weight:   308.34
Purity:   >98%
Appearance:   Greyish Purple
Chemical Name:   2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol
Solubility:   Up to 100 mM in DMSO
Synonyms:   PP242, PP 242

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Feldman et al., Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PloS Biol. 2009, 7(2), e1000038. Pubmed ID: 19209957
2. Hoang et al., Targeting TORC2 in multiple myeloma with a new mTOR kinase inhibitor. Blood, 2010, 116(22), 4560-4568. Pubmed ID: 20686120
3. Janes et al., Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nat. Med. 2010, 16, 205-213. Pubmed ID: 20072130

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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