LY364947

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LY364947

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Cat No: 13341

Biochemicals - Kinase Inhibitors

Transforming growth factor-β (TGF-β) signals through a cell surface heteromeric complex involving type I (TGF-β RI) and type II (TGF-β RII) receptors. Downstream signal transduction is mediated by the TGF-β RI kinase domain through the phosphorylation...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-quinoline

Correlated keywords:

TGF-? receptor inhibitors antagonists Smad p38 MAPK MLK7 cells growth fibroblasts NIH 3T3 cells phosphorylation fibronectin PAI-1 uPA matrigel invasion MDA-MB-231 cells transforming factors LY 364947 LY-364947 HTS-466284 HTS466284 HTS 466284 ALK5 Inhibitor I T?R-I inhibitor Transforming Growth Factor-? Type I Receptor Kinase Inhbitor [3-(Pyridin-2-yl)-4-(4-quinoynyl)]-1H-pyrazole

Product Overview:
Transforming growth factor-β (TGF-β) signals through a cell surface heteromeric complex involving type I (TGF-β RI) and type II (TGF-β RII) receptors. Downstream signal transduction is mediated by the TGF-β RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC50 value of 59 nM.{17263} LY364947 less effectively inhibits TGF-β RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and mixed-lineage kinase 7 (MLK7; IC50 = 1,400 nM).{17263,17264} It inhibits TGF-β-induced cell growth (IC50 = 89 nM) in NIH 3T3 mouse fibroblasts{17263} and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.{17265}

Size	5 mg
Shipping	dry ice
CAS Number	396129-53-6
Molecular Formula	C₁₇H₁₂N₄
SMILES	C1(C2=CC=NC3=C2C=CC=C3)=CNN=C1C4=NC=CC=C4
Molecular Weight	272,3
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.19
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.