LY-364947
LY-364947 Basic information
- 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
- 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.
- InChIKey
- IBCXZJCWDGCXQT-UHFFFAOYSA-N
Safety Information
- 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
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.3?Cell 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
References
1) Sawyer?et al. (2003),?Synthesis and activity of new aryl-and hetero-aryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain; J. Med. Chem.,?46?3953 2) Shiou?et al. (2006),?Smad4-dependent regulation of urokinase plasminogen activator secretion and RNA stability associated with invasiveness by autocrine and paracrine transforming growth factor-beta; J. Biol. Chem.,?281?33971 3) Hardee?et al. (2012),?Resistance of glioblastoma-initiating cells to radiation mediated by the tumor microenvironment can be abolished by inhibiting transforming growth factor-β; Cancer Res.,?72?4119
LY-364947Supplier
- Tel
- 17317130613
- 3358272972@qq.com
- Tel
- sales@boylechem.com
- Tel
- 010-82848833 400-666-7788
- jkinfo@jkchemical.com
- Tel
- 821-50328103-801 18930552037
- 3bsc@sina.com
- Tel
- +86-21-20908456
- sales@BioChemBest.com
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