LY364947
LY364947 structure
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Common Name | LY364947 | ||
|---|---|---|---|---|
| CAS Number | 396129-53-6 | Molecular Weight | 272.304 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 490.8±45.0 °C at 760 mmHg | |
| Molecular Formula | C17H12N4 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 268.7±15.1 °C | |
| Symbol |
GHS06, GHS09 |
Signal Word | Danger | |
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Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
J. Med. Chem. 46 , 3953-3956, (2003) Pyrazole-based inhibitors of the transforming growth factor-beta type I receptor kinase domain (TbetaR-I) are described. Examination of the SAR in both enzyme- and cell-based in vitro assays resulted in the emergence of two subseries featuring differing selec... |
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Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
J. Med. Chem. 49 , 2138-2142, (2006) Novel dihydropyrrolopyrazole-substituted benzimidazoles were synthesized and evaluated in vitro as inhibitors of transforming growth factor-beta type I receptor (TGF-beta RI), TGF-beta RII, and mixed lineage kinase-7 (MLK-7). These compounds were found to be ... |
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Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFbeta receptor kinase (TbetaRI).
Bioorg. Med. Chem. Lett. 13 , 4355-4359, (2003) We describe the discovery, using shape-based virtual screening, of a potent, ATP site-directed inhibitor of the TbetaRI kinase, an important and novel drug target for fibrosis and cancer. The first detailed report of a TbetaRI kinase small molecule co-complex... |
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Smad4-dependent regulation of urokinase plasminogen activator secretion and RNA stability associated with invasiveness by autocrine and paracrine transforming growth factor-beta.
J. Biol. Chem. 281 , 33971-33981, (2006) Metastasis is a primary cause of mortality due to cancer. Early metastatic growth involves both a remodeling of the extracellular matrix surrounding tumors and invasion of tumors across the basement membrane. Up-regulation of extracellular matrix degrading pr... |
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A TGF-β receptor 1 inhibitor for prevention of proliferative vitreoretinopathy.
Exp. Eye Res. 123 , 72-86, (2014) This study evaluates the use of the TGF-β receptor 1 inhibitor LY-364947 (LY) to prevent proliferative vitreoretinopathy (PVR). For the in vitro experiments Human Tenon's Fibroblasts (HTFs) and retinal pigment epithelial (RPE) cells were treated with differen... |
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Conditional ablation of TGF-β signaling inhibits tumor progression and invasion in an induced mouse bladder cancer model.
Sci. Rep. 6 , 29479, (2016) The role of transforming growth factor-β (TGF-β) signaling in cancer progression is still under debate. To determine the function of TGF-β signaling in bladder cancer progression, we conditionally knocked out the Tgfbr2 in mouse model after a N-butyl-N-4-hydr... |
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Expressed repeat elements improve RT-qPCR normalization across a wide range of zebrafish gene expression studies.
PLoS ONE 9(10) , e109091, (2014) The selection and validation of stably expressed reference genes is a critical issue for proper RT-qPCR data normalization. In zebrafish expression studies, many commonly used reference genes are not generally applicable given their variability in expression ... |