PP242

Drug · 3 studies in the Atlas

A lab tool drug, similar to Torin1, that blocks mTOR's active site directly. Like Torin1, it shuts down both mTOR complexes, unlike rapamycin which mainly hits one.

An ATP-competitive mTOR kinase inhibitor (a 'TORKinib'); like Torin1, inhibits both mTORC1 and mTORC2 and blocks outputs that rapamycin leaves intact.

TL;DR. PP242 appears in 3 curated studies in Oliver's mTOR Atlas: 3 at the molecular level (cells, biochemistry, structure). No study in people is recorded for it in the Atlas yet.

Which mTOR drugs are in development now, and why: mTOR drugs in development →

Evidence at a glance

Evidence	What it means	Studies
M	Molecular — cells, biochemistry, structure	3

No direct human evidence in the Atlas for this entity yet — everything below rests on animal or molecular work.

Studies

Year	Evidence	Study
2012	M	Distinct perturbation of the translatome by the antidiabetic drug metformin LAR2012 The authors compared genome-wide changes in mRNA translation caused by metformin with those caused by the mTOR inhibitors rapamycin and PP242 in cancer cells. Metformin changed gene expression at the level of translation to an extent comparable to the classic mTOR inhibitors. Its antiproliferative effect could be explained by selective suppression of translation of mRNAs encoding cell-cycle regulators, acting through the mTORC1 / 4E-BP pathway. The paper provided evidence that metformin's effect on cell growth in vitro goes through selective translational control rather than a general drop in protein synthesis. Boundary: Cultured cancer cells at drug concentrations used in vitro; does not show that metformin at clinical doses acts this way in patients. Drafted from the abstract only.
2010	M	Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor JAN2010 The ATP-competitive TORC1/2 inhibitor PP242 selectively kills leukemia cells, with much weaker effects on the proliferation and function of normal lymphocytes.
2009	M	Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2 FEL2009 The parallel discovery to Thoreen 2009 (same year), from the Shokat lab. Their TORKinibs (PP242, PP30) block mTOR's active site, hitting both complexes and shutting down cap-dependent translation that rapamycin misses. Together these two papers established a whole new drug class beyond rapamycin.

Related entities

mTORC1 3 ATP-competitive mTOR inhibitors 2 Rapamycin 2 mTORC2 2 Metformin 1 Akt/PKB 1 4E-BP1 1

Cite this page

ShowHide

Barton, O. (2026). PP242 [Entity page]. In Oliver's mTOR Atlas [Data set]. https://mtor-atlas.org/drug/pp242/ · Dataset DOI 10.5281/zenodo.22059963

@misc{atlas_drug_pp242,
  author       = {Barton, Oliver},
  title        = {{Oliver's mTOR Atlas}: PP242},
  howpublished = {Entity page in a data set},
  year         = {2026},
  url          = {https://mtor-atlas.org/drug/pp242/},
  doi          = {10.5281/zenodo.22059963}
}

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