LY 364947 A selective ATP-competitive inhibitor of TGF-β Receptor I kinase

LY 364947 (CAS 396129-53-6)

LY 364947 | CAS 396129-53-6 is rated 5.0 out of 5 by 1.
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Synonym: TGF-β RI Kinase Inhibitor; 3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole
Application: A selective ATP-competitive inhibitor of TGF-β Receptor I kinase
CAS Number: 396129-53-6
Molecular Weight: 272.3
Molecular Formula: C17H12N4
* Refer to Certificate of Analysis for lot specific data (including water content).
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LY 364947 is a diheteroaryl-substituted pyrazole compound used as a selective, ATP-competitive inhibitor of TGF-βRI (TGF-β Receptor I kinase). Studies of mouse fibroblasts show that LY 364947 inhibits cellular growth and transcription activation via TGF-β Receptor I kinase inhibition. In addition, TGF-β 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 β RII.


References

1. Kano, M.R., et al. 2009. Cancer Sci. 100: 173-180. PMID: 19037999
2. Yoshioka, N., et al. 2010. J Neurosci Res. [Epub ahead of print]. PMID: 21181763
3. Kimura-Kuroda, J., et al. 2010. Mol. Cell. Neurosci. 43: 177-187. PMID: 19897043

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), water (<1 mg/ml at 25° C), ethanol (<1 mg/ml at 25° C), DMF (~0.1 mg/ml), and 1:1 DMF:PBS (pH 7.2) (~0.5 mg/ml).
Storage :
Store at -20° C
Melting Point :
230° C (dec.)
Boiling Point :
~490.82° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.7 (Predicted)
IC50 :
TGFβ RII: IC50 = 27 nM (human); TGF-β Receptor I kinase : IC50 = 51 nM; HepG2: IC50 = 60 nM (human); NIH3T3: IC50 = 81 nM (mouse); RIPK2: IC50 = 0.11 µM
pK Values :
pKa: 8.94 (Predicted), pKb: 4.39 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
447966
MDL Number :
MFCD00800758
SMILES :
N1C=C(C(=N1)C1=NC=CC=C1)C1=CC=NC2=C1C=CC=C2

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LY 364947  Product Citations

See how others have used LY 364947. Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 27378170  Liang, Y. et al. 2016. Sci Rep. 6: 29479.

PMID: # 25862758  Patel, BB. et al. 2015. Toxicol. Sci. 146: 101-15.

PMID: # 25752153  Ontogenez. 45: 355-60.

PMID: # 25715600  Ermakov, AM. et al. Biofizika. 59: 552-7.

Citations 1 to 4 of 4 total

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 Nassar Nassar, 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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