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Submit ReviewLY 364947
Description: Selective inhibitor of TGF-βRI
Alternative Names: HTS 466284
Chemical Name: 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline
Purity: ≥99% (HPLC)
Biological Activity for LY 364947
LY 364947 is a 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 for LY 364947
LY 364947 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for LY 364947
| 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 for LY 364947
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.23 | 100 |
Preparing Stock Solutions for LY 364947
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.
| 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 for LY 364947
References for LY 364947
References are publications that support the biological activity of the product.
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 urok. 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.
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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:
Yumoto et al (2016) Axl is required for TGF-β2-induced dormancy of prostate cancer cells in the bone marrow. Sci Rep 6 36520 PMID: 27819283
Wang et al (2017) NKCC1 up-regulation contributes to early post-traumatic seizures and increased post-traumatic seizure susceptibility. Brain Struct Funct 222 1543 PMID: 27586142
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
Ameri et al (2019) 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. Int J Mol Sci 20 PMID: 31336560
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
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
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
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
Hough et al (2012) Tgf-β induced Erk phosphorylation of smad linker region regulates smad signaling. Invest Ophthalmol Vis Sci 7 e42513 PMID: 22880011
Do you know of a great paper that uses LY 364947 from Tocris? Please let us know.
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Pathways for LY 364947
