Skip to Content
Merck
All Photos(1)

Documents

Safety Information

475988

Sigma-Aldrich

mTOR Inhibitor III, PP242

The mTOR Inhibitor III, PP242 controls the biological activity of mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

mTOR Inhibitor III, PP242, 2-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol, Dihydrate, TORKinib, mTOR Inhibitor III, PP242

Sign Into View Organizational & Contract Pricing
All Photos(1)

About This Item

Empirical Formula (Hill Notation):
C16H16N6O · 2H2O
Molecular Weight:
344.37
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 100 mg/mL

shipped in

wet ice

storage temp.

−20°C

General description

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 µM 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 µM (maximum of 68% or 77% inhibition observed with 10 or 100 µM ATP, respectively). PP242 differentially inhibits insulin-stimulated phosphorylations of cellular proteins both in cultures (2.5 µM) 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 (Cat. Nos. 553210, 553211, 553212), 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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Feldman, M.E., et al. 2009. PLoS Biology7, 391.
Apsel, B., et al. 2008. Nat. Chem. Biol.4, 691.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

JAN Code

475988-MG:
475988-5MG:

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Vincent Picher-Martel et al.
International journal of molecular sciences, 24(6) (2023-03-30)
Amyotrophic lateral sclerosis (ALS) is a clinically highly heterogeneous disease with a survival rate ranging from months to decades. Evidence suggests that a systemic deregulation of immune response may play a role and affect disease progression. Here, we measured 62
Aydan C H Szeto et al.
Nature immunology, 24(1), 123-135 (2022-12-23)
Naive CD4+ T lymphocytes initially undergo antigen-specific activation to promote a broad-spectrum response before adopting bespoke cytokine expression profiles shaped by intercellular microenvironmental cues, resulting in pathogen-focused modular cytokine responses. Interleukin (IL)-4-induced Gata3 upregulation is important for the helper type
Dhiman Sankar Pal et al.
Developmental cell, 58(13), 1170-1188 (2023-05-24)
Ras signaling is typically associated with cell growth, but not direct regulation of motility or polarity. By optogenetically targeting different nodes in the Ras/PI3K/Akt network in differentiated human HL-60 neutrophils, we abruptly altered protrusive activity, bypassing the chemoattractant receptor/G-protein network.
Spatiotemporal dynamics of membrane surface charge regulates cell polarity and migration.
Banerjee, et al.
Nature Cell Biology, 24, 1499-1515 (2023)
Liu Liu et al.
Science signaling, 15(715), eabh2290-eabh2290 (2022-01-05)
The kinase AKT (also known as protein kinase B) is a key regulator of cell proliferation, survival, and metabolism. In addition to being activated by growth factors, AKT is activated in response to DNA damage. Here, we found that the
View All Related Papers

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service