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P0037

Sigma-Aldrich

PP242 hydrate

≥98% (HPLC), powder

Synonym(s):

2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol

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About This Item

Empirical Formula (Hill Notation):
C16H16N6O · xH2O
CAS Number:
1173019-76-5
Molecular Weight:
308.34 (anhydrous basis)
MDL number:
MFCD12828866
UNSPSC Code:
12352200
PubChem Substance ID:
329819988
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

off-white

solubility

DMSO: >10 mg/mL

storage temp.

2-8°C

SMILES string

O.CC(C)n1nc(-c2cc3cc(O)ccc3[nH]2)c4c(N)ncnc14

InChI

1S/C16H16N6O.H2O/c1-8(2)22-16-13(15(17)18-7-19-16)14(21-22)12-6-9-5-10(23)3-4-11(9)20-12;/h3-8,20,23H,1-2H3,(H2,17,18,19);1H2

InChI key

FMDOLJSFPXFBIL-UHFFFAOYSA-N

Application

PP242 hydrate has been used:
  • as a mammalian target of rapamycin (mTOR) inhibitor to study its effects on rat fibroblast mTOR complex 1 and 2 (mTORC1 & 2) signaling
  • as an mTOR inhibitor to treat mouse embryonic fibroblasts (MEF) and cumulus cells (CCs) to study its effects on reactivation of embryonic nucleoli and ribosome biogenesis
  • as a target of rapamycin (TOR) kinase inhibitor for the treatment of Arabidopsis to study its effects against Fusarium graminearum infection

Biochem/physiol Actions

PP242 is a potent and selective mTOR inhibitor. PP242 is a first selective inhibitor that targets ATP domain of mTOR.

Features and Benefits

This compound is featured on the PKB/Akt page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

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’.

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Min Liu et al.
Biochemical and biophysical research communications, 463(3), 255-261 (2015-05-24)
Activation of quiescent hepatic stellate cells (HSCs) is the central event of liver fibrosis. The translational machinery is an optimized molecular network that affects cellular homoeostasis and diseases, whereas the role of protein translation in HSCs activation and liver fibrosis
TOR signaling downregulation increases resistance to the cereal killer Fusarium graminearum
Aznar N, et al.
Plant signaling & behavior, 13(2), e1414120-e1414120 (2018)
Transient inhibition of rDNA transcription in donor cells improves ribosome biogenesis and preimplantation development of embryos derived from somatic cell nuclear transfer
Liao C, et al.
Faseb Journal, 26(12), 2774-2789 (2020)
Piero Dalle Pezze et al.
Autophagy, 17(5), 1131-1141 (2020-04-23)
During macroautophagy/autophagy, the ULK complex nucleates autophagic precursors, which give rise to autophagosomes. We analyzed, by live imaging and mathematical modeling, the translocation of ATG13 (part of the ULK complex) to the autophagic puncta in starvation-induced autophagy and ivermectin-induced mitophagy.
Jigang Wang et al.
Nature protocols, 12(2), 279-288 (2017-01-13)
At present, several assays that use radioisotope labeling to quantify the degradation of long-lived proteins have been developed to measure autophagic flux. Here, we describe a nonradioactive pulse-chase protocol using L-azidohomoalanine (AHA) labeling to quantify long-lived protein degradation during autophagy.
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