- LY-364947
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- $59.00
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2026-07-27
- CAS:396129-53-6
- Purity: 99.71%
- Supply Ability: 10g
- LY-364947
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2024-11-01
- CAS:396129-53-6
- Min. Order: 1g
- Purity: 98%
- Supply Ability: 1000kgs
- LY-364947
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- $1.00
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2019-09-06
- CAS:396129-53-6
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 20kg
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| Product Name: | LY-364947 | | Synonyms: | [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole;4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline;LY364947(HTS 466284);E 616451;HTS 466284;2-[4-(Quinolin-4-yl)-1H-pyrazol-3-yl]pyridine, 3-(Pyridin-2-yl)-4-(quinolin-4-yl)-1H-pyrazole;Quinoline, 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-;4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline E 616451 | | CAS: | 396129-53-6 | | MF: | C17H12N4 | | MW: | 272.3 | | EINECS: | | | Product Categories: | API;Inhibitors;Smad;TGF-beta | | Mol File: | 396129-53-6.mol |  |
| | LY-364947 Chemical Properties |
| Melting point | >230℃ (dec.) | | Boiling point | 490.8±45.0 °C(Predicted) | | density | 1.283±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: soluble2mg/mL, clear | | pka | 8.94±0.50(Predicted) | | form | powder | | color | white to beige | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. | | 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) | | InChIKey | IBCXZJCWDGCXQT-UHFFFAOYSA-N | | SMILES | N1C2C(=CC=CC=2)C(C2=CNN=C2C2=NC=CC=C2)=CC=1 |
| Hazard Codes | T,N | | Risk Statements | 25-36/37/38-50/53 | | Safety Statements | 26-45-60-61 | | RIDADR | UN 2811 6.1/PG 3 | | WGK Germany | 3 | | HS Code | 2933491090 | | Storage Class | 11 - Combustible Solids |
| | LY-364947 Usage And Synthesis |
| Description | LY-364947 (396129-53-6) is a selective ALK5 inhibitor, IC50 = 59, 400 and 1400 nM for TGF-β RI, TGF-β RII and MLK-7K, respectively.1 Inhibits Smad2 phosphorylation induced by TGF-β as well as fibronectin expression and MDA-MB-231 cell invasion.2 LY-364947 abolishes resistance of glioblastoma-initiating cells to radiation.3Cell permeable. | | Uses | LY 364947, is a potent ATP-competitive inhibitor of Tgf-b signaling. | | Definition | ChEBI: LY 364947 is a member of the class of pyrazoles carrying pyridin-2-yl and quinolin-4-yl substituents at positions 3 and 4 respectively. It has a role as a TGFbeta receptor antagonist. It is a member of pyrazoles, a member of pyridines and a member of quinolines. | | Biological Activity | Selective inhibitor of TGF- β type-I receptor (TGF- β RI, TGFR-I, T β R-I, ALK-5) (IC 50 values are 59, 400 and 1400 nM for TGR- β RI, TGF- β RII and MLK-7K respectively). Inhibits TGF- β -dependent luciferase production in mink lung cells (p3TP lux) and growth in mouse fibroblasts (NIH 3T3) (IC 50 values are 47 and 89 nM respectively). Suppresses invasion of MDA-MB-231 breast cancer cells in a matrigel invasion assay. | | Biochem/physiol Actions | LY-364947 is a selective, ATP-competitive inhibitor of Transforming Growth Factor-β Type I receptor kinase (TGF-β RI, ALK5) with IC50 = 59 nM. It is much less potent at related kinases, with IC50 = 400 nM for TGF-β RII and IC50 = 1400 nM for mixed lineage kinase-7 (MLK-7), a kinase in the MAP kinase signal pathway and closely related to TGF-β RII. LY-364947 inhibits TGF-β-dependent cellular growth (IC50 = 81 nM) in NIH 3T3 mouse fibroblasts. | | in vitro | ly364947 was quickly identified as a potent inhibitor (ic50= 51 nm) and was chosen as a platform for sar development. compounds were further evaluated as inhibitors of tgf-β-dependent luciferase production in mink lung cells (p3tp lux) and growth in mouse fibroblasts (nih 3t3) [1]. | | in vivo | in a rat model of nmda-induced retinal degeneration, simultaneous injection of nmda and the tgf-β inhibitor ly364947 slightly but significantly attenuated the reduction in number of cells in the ganglion cell layer and almost completely prevented the enhancement of capillary degeneration. [3]. | | storage | Store at RT | | Background | LY-364947, also known as HTS-466284, is a potent and selective TGF-β type-I receptor inhibitor. This small molecule specifically targets TGF-β RI with an IC50 value of 59 nM and is less effective on TGF-β RII and MLK-7K. LY-364947 regulates MDA-MB-231 cell invasion by inhibiting autocrine TGF-β signaling. Patients in intensive care units that suffer from chronic sepsis can experience weakening of the diaphragm muscles caused by muscle wasting, requiring mechanical ventilation. Members of the TGF-β family can trigger the activation of protein breakdown. Inhibition of the TGF-β pathway can protect the diaphragm during chronic sepsis, making LY-364947 an interesting compound to study as it relates to effective ICU patient care. | | References | [1] J. SCOTT SAWYER. Synthesis and Activity of New Aryl- and Heteroaryl-Substituted Pyrazole Inhibitors of the Transforming Growth Factor-β Type I Receptor Kinase Domain[J]. Journal of Medicinal Chemistry, 2003, 46 19: 3953-3956. DOI:10.1021/jm0205705
[2] SHENG-RU SHIOU. Smad4-dependent regulation of urokinase plasminogen activator secretion and RNA stability associated with invasiveness by autocrine and paracrine transforming growth factor-beta.[J]. The Journal of Biological Chemistry, 2006, 281 45: 33971-33981. DOI:10.1074/jbc.m607010200
[3] MATTHEW E HARDEE. Resistance of glioblastoma-initiating cells to radiation mediated by the tumor microenvironment can be abolished by inhibiting transforming growth factor-β.[J]. Cancer research, 2012, 72 16: 4119-4129. DOI:10.1158/0008-5472.can-12-0546 |
| | LY-364947 Preparation Products And Raw materials |
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