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LY 364947 (CAS 396129-53-6)

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Alternate Names:
TGF-β RI Kinase Inhibitor; 3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole
Application:
LY 364947 is a selective ATP-competitive inhibitor of TGF-β Receptor I kinase
CAS Number:
396129-53-6
Molecular Weight:
272.3
Molecular Formula:
C17H12N4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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LY 364947 is a diheteroaryl-substituted pyrazole compound used as a selective, ATP-competitive inhibitor of TGF-betaRI (TGF-beta Receptor I kinase). Studies of mouse fibroblasts show that LY 364947 inhibits cellular growth and transcription activation via TGF-beta Receptor I kinase inhibition. In addition, TGF-beta Receptor I kinase is responsible for fibroblast proliferation and the accumulation of astrocytes around the fibrotic scar when injury occurs to cells. In vitro studies report that in the presence of LY 364947 the amount of reactive astrocytes at the lesion site is also reduced. Furthermore, studies show that LY 364947 strongly effects intraplug vasculature by increasing the extravasation of Dextran (sc-218165). LY 364947 is an inhibitor of eIF2 alpha, MLTK, p38 alpha and TGF beta RII.


LY 364947 (CAS 396129-53-6) References

  1. Comparison of the effects of the kinase inhibitors imatinib, sorafenib, and transforming growth factor-beta receptor inhibitor on extravasation of nanoparticles from neovasculature.  |  Kano, MR., et al. 2009. Cancer Sci. 100: 173-80. PMID: 19037999
  2. An in vitro model of the inhibition of axon growth in the lesion scar formed after central nervous system injury.  |  Kimura-Kuroda, J., et al. 2010. Mol Cell Neurosci. 43: 177-87. PMID: 19897043
  3. Small molecule inhibitor of type I transforming growth factor-β receptor kinase ameliorates the inhibitory milieu in injured brain and promotes regeneration of nigrostriatal dopaminergic axons.  |  Yoshioka, N., et al. 2011. J Neurosci Res. 89: 381-93. PMID: 21259325
  4. The specificities of small molecule inhibitors of the TGFß and BMP pathways.  |  Vogt, J., et al. 2011. Cell Signal. 23: 1831-42. PMID: 21740966
  5. Stromal fibroblast-bone marrow-derived cell interactions: implications for myofibroblast development in the cornea.  |  Singh, V., et al. 2012. Exp Eye Res. 98: 1-8. PMID: 22465408
  6. Transforming growth factor-beta1 induces microvascular abnormalities through a down-modulation of neural cell adhesion molecule in human hepatocellular carcinoma.  |  Balzarini, P., et al. 2012. Lab Invest. 92: 1297-309. PMID: 22732936
  7. Enhanced effectivity of an ALK5-inhibitor after cell-specific delivery to hepatic stellate cells in mice with liver injury.  |  van Beuge, MM., et al. 2013. PLoS One. 8: e56442. PMID: 23441194
  8. Validated RP-HPLC method for the simultaneous analysis of gemcitabine and LY-364947 in liposomal formulations.  |  Bansal, SS., et al. 2013. Curr Drug Targets. 14: 1061-9. PMID: 23721184
  9. A TGF-β receptor 1 inhibitor for prevention of proliferative vitreoretinopathy.  |  Nassar, K., et al. 2014. Exp Eye Res. 123: 72-86. PMID: 24742493
  10. HDAC Inhibitor-Mediated Epigenetic Regulation of Glaucoma-Associated TGFβ2 in the Trabecular Meshwork.  |  Bermudez, JY., et al. 2016. Invest Ophthalmol Vis Sci. 57: 3698-707. PMID: 27403998
  11. Wulong Xiaozheng Wan medicated serum inhibits epithelial-mesenchymal transition in human gastric carcinoma cell line BGC823 by modulation of transforming growth factor-β1/Smad signaling.  |  Zhang, Y., et al. 2019. J Tradit Chin Med. 39: 380-392. PMID: 32186010
  12. Low-Field Magnetic Stimulation Accelerates the Differentiation of Oligodendrocyte Precursor Cells via Non-canonical TGF-β Signaling Pathways.  |  Dolgova, N., et al. 2021. Mol Neurobiol. 58: 855-866. PMID: 33037982
  13. Silencing SIX1 inhibits epithelial mesenchymal transition through regulating TGF-β/Smad2/3 signaling pathway in papillary thyroid carcinoma.  |  Min, WP. and Wei, XF. 2021. Auris Nasus Larynx. 48: 487-495. PMID: 33077306

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

LY 364947, 5 mg

sc-203122
5 mg
$105.00

LY 364947, 10 mg

sc-203122A
10 mg
$153.00

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. LY 364947, sc-203122, is in light yellow powder form.
Answered by: Chemical Support 4
Date published: 2017-06-28
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Rated 5 out of 5 by from NassarNassar, K. et al. (PubMed 24742493) evaluated the use of the TGF- receptor 1 inhibitor LY 364947 to prevent proliferative vitreoretinopathy (PVR). They found that LY 364947 reduces Human Tenon's Fibroblast proliferation and retinal pigment epithelial transdifferentiation in vitro and prevents proliferative vitreoretinopathy and subsequent tractional retinal detachment in vivo. -SCBT Publication Review
Date published: 2015-04-07
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LY 364947 is rated 5.0 out of 5 by 1.
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