LY 364947

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Cat.No. 2718 - LY 364947 | C17H12N4 | CAS No. 396129-53-6
Description: Selective inhibitor of TGF-βRI
Alternative Names: HTS 466284
Chemical Name: 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline
Purity: ≥99% (HPLC)
Datasheet
Citations (8)
Literature
Pathways

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.

Compound Libraries

LY 364947 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 272.31
Formula C17H12N4
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 396129-53-6
PubChem ID 447966
InChI Key IBCXZJCWDGCXQT-UHFFFAOYSA-N
Smiles N1C=C(C(=N1)C1=CC=CC=N1)C1=CC=NC2=CC=CC=C12

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 27.23 100

Preparing Stock Solutions

The following data is based on the product molecular weight 272.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.67 mL 18.36 mL 36.72 mL
5 mM 0.73 mL 3.67 mL 7.34 mL
10 mM 0.37 mL 1.84 mL 3.67 mL
50 mM 0.07 mL 0.37 mL 0.73 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Sawyer et al (2003) Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-μ type I receptor kinase domain. J.Med.Chem. 46 3953 PMID: 12954047

Li et al (2006) 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. J.Med.Chem. 49 2138 PMID: 16539403

Shiou et al (2006) Smad4-dependent regulation of urokinase plasminogen activator secretion and RNA stability associated with invasiveness by autocrine and paracrine transforming growth factor-β. J.Biol.Chem. 281 33971 PMID: 16959768


If you know of a relevant reference for LY 364947, please let us know.

View Related Products by Product Action

View all TGF-β Receptor Inhibitors

Keywords: Selective inhibitors inhibits TGF-βRI TGF-β TGF-betaRI TGFbRI TGFbR1 tgf-b1Transforming Growth Factors Beta Receptors TGF-beta Receptor Serine/Threonine Kinases RSTKs LY364947 HTS466284 HTS 466284 TGF-beta Receptors

8 Citations for LY 364947

Citations are publications that use Tocris products. Selected citations for LY 364947 include:

Oruqaj et al (2015) Compromised peroxisomes in idiopathic pulmonary fibrosis, a vicious cycle inducing a higher fibrotic response via TGF-β signaling. Proc Natl Acad Sci U S A 112 E2048 PMID: 25848047

Oshimori et al (2015) TGF-β promotes heterogeneity and drug resistance in squamous cell carcinoma. Cell 160 963 PMID: 25723170

Jajosky et al (2014) RepSox slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression. Stem Cells Transl Med 3 836 PMID: 24855276

Oerlecke et al (2013) Cyclic AMP enhances TGFβ responses of breast cancer cells by upregulating TGFβ receptor I expression. PLoS One 8 e54261 PMID: 23349840

Sethi et al (2013) Gremlin utilizes canonical and non-canonical TGFβ signaling to induce lysyl oxidase (LOX) genes in human trabecular meshwork cells. Invest Ophthalmol Vis Sci 113 117 PMID: 23748100

Hough et al (2012) Tgf-β induced Erk phosphorylation of smad linker region regulates smad signaling. Invest Ophthalmol Vis Sci 7 e42513 PMID: 22880011

Sethi et al (2011) Transforming growth factor-β induces extracellular matrix protein cross-linking lysyl oxidase (LOX) genes in human trabecular meshwork cells. Nat Commun 52 5240 PMID: 21546528

Sethi et al (2011) Role of TGFβ/Smad signaling in gremlin induction of human trabecular meshwork extracellular matrix proteins. PLoS One 52 5251 PMID: 21642622


Do you know of a great paper that uses LY 364947 from Tocris? If so please let us know.

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Stem Cells

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Pathways for LY 364947

TGF-β

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.

Protocols

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