PI 103 hydrochloride
Chemical Name: 3-[4-(4-Morpholinylpyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol hydrochloride
Purity: ≥98%
Biological Activity
PI 103 hydrochloride is an inhibitor of DNA-PK, PI 3-kinase (p110α) and mTOR (IC50 values are 2, 8, 20, 26, 48, 83, 88, 150, 850, 920, ~ 1000 and 2300 nM for DNA-PK, p110α, mTORC1, PI 3-KC2β, p110δ, mTORC2, p110β, p110γ, ATR, ATM, PI 3-KC2α and hsVPS34 respectively). Inhibits growth of human tumor xenografts in mice in vivo. Induces autophagosome formation in glioma cells.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Platelet-Derived Growth Factor CC-Mediated Neuroprotection against HIV Tat Involves TRPC-Mediated Inactivation of GSK 3beta.
Peng F, Yao H, Akturk H, Buch S
PLoS ONE, 2012;7(10):e47572. -
The transcriptional regulator NAB2 reveals a two-step induction of TRAIL in activated plasmacytoid DCs.
Balzarolo M, Karrich J, Engels S, Blom B, Medema J, Wolkers M
Eur J Immunol, 2012;42(11):3019-27. -
Insulin-like growth factor promotes cardiac lineage induction in vitro by selective expansion of early mesoderm.
Engels M, Rajarajan K, Feistritzer R, Sharma A, Nielsen U, Schalij M, de Vries A, Pijnappels D, Wu S
Stem Cells, 2014;32(6):1493-502. -
Cytokine-induced loss of glucocorticoid function: effect of kinase inhibitors, long-acting beta(2)-adrenoceptor [corrected] agonist and glucocorticoid receptor ligands.
Rider C, Shah S, Miller-Larsson A, Giembycz M, Newton R
PLoS ONE, 2015;10(1):e0116773. -
A pharmacological map of the PI3-K family defines a role for p110α in Ins signaling.
Knight et al.
Cell, 2006;125:733 -
A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma.
Fan et al.
Cancer cell, 2006;9:341 -
Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositol 3-kinase.
Raynaud et al.
Cancer Res., 2007;67:5840 -
Akt and autophagy cooperate to promote survival of drug-resistant glioma.
Fan et al.
Sci.Signal., 2010;3:ra81
Product Datasheets
Citations for PI 103 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for PI 103 hydrochloride include:
10 Citations: Showing 1 - 10
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Single-Cell RNA-Sequencing-Based CRISPRi Screening Resolves Molecular Drivers of Early Human Endoderm Development.
Authors: Genga Et al.
Cell Rep 2019;27:708
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Capacitation of human na�ve pluripotent stem cells for multi-lineage differentiation.
Authors: Rostovskaya Et al.
Development 2019;146
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Epigenetic resetting of human pluripotency.
Authors: Guo Et al.
Development 2017;144:2748
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Rapamycin-insensitive up-regulation of adipocyte phospholipase A2 in tuberous sclerosis and lymphangioleiomyomatosis.
Authors: Li Et al.
J Exp Med 2014;9:e104809
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Mitogen-activated protein kinase-interacting kinase regulates mTOR/AKT signaling and controls the serine/arginine-rich protein kinase-responsive type 1 internal ribosome entry site-mediated translation and viral oncolysis.
Authors: Brown Et al.
PLoS One 2014;88:13149
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OE and mTORC2 cooperate to enhance prostaglandin biosynthesis and tumorigenesis in TSC2-deficient LAM cells.
Authors: Li Et al.
Pain 2014;211:15
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P-Rex1 cooperates with PDGFRβ to drive cellular migration in 3D microenvironments.
Authors: Campbell Et al.
PLoS One 2013;8:e53982
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ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change.
Authors: Montané and Menand
J Virol 2013;64:4361
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Platelet-derived growth factor CC-mediated neuroprotection against HIV Tat involves TRPC-mediated inactivation of GSK 3beta.
Authors: Peng Et al.
PLoS One 2012;7:e47572
-
A screen for regulators of survival of motor neuron protein levels.
Authors: Makhortova Et al.
Nat Chem Biol 2011;7:544
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