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pp242

pp242 Unit size Cat. code Docs Qty Price
mTOR inhibitor
5 mg
inh-pp242
+-
$162.00

mTOR inhibitor

pp242 (also known as Torkinib) is a potent, selective and ATP‑competitive inhibitor of mTOR (mammalian target of rapamycin) kinase, a key protein kinase of the PI3K/AKT signaling pathway that plays a central role in controlling cell growth, proliferation, and survival.

mTOR is a major negative regulatory axis of autophagy. Thus, pp242 is an effective inducer of autophagy [1].

Specifically, pp242 is able to induce autophagy by inhibiting the two mTOR-containing complexes (mTORC1 and mTORC2), neither of which is fully blocked by classical mTOR inhibitors such as rapamycin [2-4].

 

Zhou J. et al., 2013. Activation of lysosomal function in the course of autophagy via mTORC1 suppression and autophagosome-lysosome fusion. Cell Res. 23(4):508-23.
Feldman, ME. et al., 2009. Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol. 7:371-83.
Shao H. et al., 2009. Dual targeting of mTORC1/C2 complexes enhances histone deacetylase inhibitor-mediated anti-tumor efficacy in primary HCC cancer in vitro and in vivo. J. Hepatol. 56(1):176-83.
Janes MR. et al., 2010. Effective and selective targeting of Ph+ leukemia cells using a TORC1/2 kinase inhibitor. Nat Med. 16(2):205-213.

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Specifications

Working concentration: 50-400 nM (Fibroblasts and solid tumor cell lines) , 1 µM (MEF).

Purity: >97% (HPLC)

Solubility: 62 mg/ml (201.1 mM) in DMSO. 18 mg/ml (58.4 mM) in ethanol.

CAS number: 1092351-67-1

Formula: C16H16N6O

Molecular weight: 308.3

Quality control:

  • The absence of bacterial contamination (e.g. lipoproteins and endotoxins) is confirmed using HEK-Blue™ TLR2 and HEK-Blue™ TLR4 cells.
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Contents

pp242 is provided lyophilized.

  • 5 mg of pp242

pp242 is shipped at room temperature.

Store at -20 °C.

Lyophilized pp242 is stable for 2 years when properly stored.

Upon resuspension, prepare aliquots of pp242 and store at -20 °C. Resuspended pp242 is stable for 6 months when properly stored.

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