LY 364947
Chemical Name: 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline
Purity: ≥99%
Biological Activity
Selective inhibitor of TGF-β type-I receptor (TGF-β RI, TGFR-I, TβR-I, ALK-5) (IC50 values are 59, 400 and 1400 nM for TGR-β RI, TGF-β RII and MLK-7K respectively). Inhibits TGF-β-dependent luciferase production in mink lung cells (p3TP lux) and growth in mouse fibroblasts (NIH 3T3) (IC50 values are 47 and 89 nM respectively). Suppresses invasion of MDA-MB-231 breast cancer cells in a matrigel invasion assay.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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Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-μ type I receptor kinase domain.
Sawyer et al.
J.Med.Chem., 2003;46:3953 -
Dihydropyrrolopyrazole transforming growth factor-β type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-β type II receptor kinase and mixed lineage kinase 7.
Li et al.
J.Med.Chem., 2006;49:2138 -
Smad4-dependent regulation of urok. plasminogen activator secretion and RNA stability associated with invasiveness by autocrine and paracrine transforming growth factor-β.
Shiou et al.
J.Biol.Chem., 2006;281:33971
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Citations for LY 364947
The citations listed below are publications that use Tocris products. Selected citations for LY 364947 include:
11 Citations: Showing 1 - 10
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Cell Type-Specific TGF-β Mediated EMT in 3D and 2D Models and Its Reversal by TGF-β Receptor Kinase Inhibitor in Ovarian Cancer Cell Lines.
Authors: Ameri Et al.
Int J Mol Sci 2019;20
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NKCC1 up-regulation contributes to early post-traumatic seizures and increased post-traumatic seizure susceptibility.
Authors: Wang Et al.
Brain Struct Funct 2017;222:1543
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Axl is required for TGF-β2-induced dormancy of prostate cancer cells in the bone marrow.
Authors: Yumoto Et al.
Sci Rep 2016;6:36520
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TGF-β promotes heterogeneity and drug resistance in squamous cell carcinoma.
Authors: Oshimori Et al.
Cell 2015;160:963
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Compromised peroxisomes in idiopathic pulmonary fibrosis, a vicious cycle inducing a higher fibrotic response via TGF-β signaling.
Authors: Oruqaj Et al.
Proc Natl Acad Sci U S A 2015;112:E2048
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RepSox slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression.
Authors: Jajosky Et al.
Stem Cells Transl Med 2014;3:836
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Cyclic AMP enhances TGFβ responses of breast cancer cells by upregulating TGFβ receptor I expression.
Authors: Oerlecke Et al.
PLoS One 2013;8:e54261
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Gremlin utilizes canonical and non-canonical TGFβ signaling to induce lysyl oxidase (LOX) genes in human trabecular meshwork cells.
Authors: Sethi Et al.
Invest Ophthalmol Vis Sci 2013;113:117
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Tgf-β induced Erk phosphorylation of smad linker region regulates smad signaling.
Authors: Hough Et al.
Invest Ophthalmol Vis Sci 2012;7:e42513
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Role of TGFβ/Smad signaling in gremlin induction of human trabecular meshwork extracellular matrix proteins.
Authors: Sethi Et al.
PLoS One 2011;52:5251
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Transforming growth factor-β induces extracellular matrix protein cross-linking lysyl oxidase (LOX) genes in human trabecular meshwork cells.
Authors: Sethi Et al.
Nat Commun 2011;52:5240
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