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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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L129343-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $73.90 | |
L129343-10mg | 10mg | In stock | $92.90 | |
L129343-50mg | 50mg | In stock | $323.90 |
Potent, selective ATP-competitive TGFβ receptor kinase I inhibitor
Synonyms | SB19489 | 4-(3-PYRIDIN-2-YL-1H-PYRAZOL-4-YL)QUINOLINE | s2805 | HMS3229M09 | PY1 | 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline | 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-quinoline | Q-102724 | SCHEMBL21233972 | PS-7269 | BCP9000886 | GTPL6050 | LY364947 | LY- |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | 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 |
Storage Temp | Store at 2-8°C |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of transforming growth factor beta receptor 1 |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Toxic, refer to SDS for further information. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, shows 7-fold selectivity over TGFβR-II. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 4-(5-pyridin-2-yl-1H-pyrazol-4-yl)quinoline |
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INCHI | InChI=1S/C17H12N4/c1-2-6-15-13(5-1)12(8-10-19-15)14-11-20-21-17(14)16-7-3-4-9-18-16/h1-11H,(H,20,21) |
InChi Key | IBCXZJCWDGCXQT-UHFFFAOYSA-N |
Canonical SMILES | C1=CC=C2C(=C1)C(=CC=N2)C3=C(NN=C3)C4=CC=CC=N4 |
Isomeric SMILES | C1=CC=C2C(=C1)C(=CC=N2)C3=C(NN=C3)C4=CC=CC=N4 |
WGK Germany | 3 |
PubChem CID | 447966 |
Molecular Weight | 272.3 |
PubChem CID | 447966 |
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DrugBank Ligand | DB03921 |
ChEMBL Ligand | CHEMBL261454 |
CAS Registry No. | 396129-53-6 |
RCSB PDB Ligand | PY1 |
Enter Lot Number to search for COA:
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). |
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Melt Point(°C) | 230°C |
Pictogram(s) | GHS06, GHS09 |
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Signal | Danger |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H301:Toxic if swallowed H400:Very toxic to aquatic life |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P273:Avoid release to the environment. P301+P310:IF SWALLOWED: Immediately call a POISON CENTER/doctor/... |
WGK Germany | 3 |
1. Xiong Zhang, Chen Feng, Yimao Li, Chenlin Su, Shuxin Zhao, Shengdi Su, Feng Yu, Ji LI. (2021) An investigation on nephrotoxicity of Aristolactam I induced epithelial-mesenchymal transition on HK-2 cells. TOXICON, 201 (21). [PMID:34391786] [10.1016/j.toxicon.2021.08.005] |
2. Ji Li, Mincheng Zhang, Yong Mao, Yimao Li, Xiaoxia Zhang, Xuehan Peng, Feng Yu. (2018) The potential role of aquaporin 1 on aristolochic acid I induced epithelial mesenchymal transition on HK-2 cells. JOURNAL OF CELLULAR PHYSIOLOGY, 233 (6): (4919-4925). [PMID:29215709] [10.1002/jcp.26310] |
1. Yang W et al.. (2018) A mediator of phosphorylated Smad2/3, evodiamine, in the reversion of TAF-induced EMT in normal colonic epithelial cells.. Invest New Drugs, [PMID:30488243] |
2. Huang C et al.. (2020) Berberine inhibits epithelial-mesenchymal transition and promotes apoptosis of tumour-associated fibroblast-induced colonic epithelial cells through regulation of TGF-ß signalling.. J Cell Commun Signal, 14 (53-66). [PMID:31399854] |
3. Huang C et al.. (2018) Berberine reversed the epithelial-mesenchymal transition of normal colonic epithelial cells induced by SW480 cells through regulating the important components in the TGF-ß pathway.. J Cell Physiol, [PMID:30536375] |
4. Zhang X et al.. (2021) Carbon nanotubes promote alveolar macrophages toward M2 polarization mediated epithelial-mesenchymal transition and fibroblast-to-myofibroblast transdifferentiation.. Nanotoxicology, 15 (5): (588-604). [PMID:33840345] |
5. Wang XL & Huang C. (2019) Difference of TGF-ß/Smads signaling pathway in epithelial-mesenchymal transition of normal colonic epithelial cells induced by tumor-associated fibroblasts and colon cancer cells.. Mol Biol Rep, [PMID:30835040] |
6. Shan L et al.. (2018) Epigallocatechin gallate improves airway inflammation through TGF-ß1 signaling pathway in asthmatic mice.. Mol Med Rep, 18 (2): (2088-2096). [PMID:29916550] |
7. Chen K et al.. (2018) Epigallocatechingallate attenuates myocardial injury in a mouse model of heart failure through TGF-ß1/Smad3 signaling pathway.. Mol Med Rep, 17 (6): (7652-7660). [PMID:29620209] |
8. Xiong Zhang, Chen Feng, Yimao Li, Chenlin Su, Shuxin Zhao, Shengdi Su, Feng Yu, Ji LI. (2021) An investigation on nephrotoxicity of Aristolactam I induced epithelial-mesenchymal transition on HK-2 cells. TOXICON, 201 (21). [PMID:34391786] [10.1016/j.toxicon.2021.08.005] |
9. Ji Li, Mincheng Zhang, Yong Mao, Yimao Li, Xiaoxia Zhang, Xuehan Peng, Feng Yu. (2018) The potential role of aquaporin 1 on aristolochic acid I induced epithelial mesenchymal transition on HK-2 cells. JOURNAL OF CELLULAR PHYSIOLOGY, 233 (6): (4919-4925). [PMID:29215709] [10.1002/jcp.26310] |