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 (11)
Reviews
Literature (6)
Pathways (1)

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 2.0 Max and Tocriscreen Kinase Inhibitor Toolbox. 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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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 the degree 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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View Related Products by Product Action

View all TGF-β Receptor Inhibitors

Keywords: LY 364947, LY 364947 supplier, 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, 2718, Tocris Bioscience

11 Citations for LY 364947

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

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

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

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


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

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Kinases Product Listing

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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.

Stem Cells

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.

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.