LY-364947
- Product Name
- LY-364947
- CAS No.
- 396129-53-6
- Chemical Name
- LY-364947
- Synonyms
- CS-576;Y364947;E 616451;LY-364947;HTS 466284;LY-364947, >=98%;LY 364947;LY-364947;LY-364947 USP/EP/BP;LY364947(HTS 466284);LY-364947, 396129-53-6
- CBNumber
- CB3972214
- Molecular Formula
- C17H12N4
- Formula Weight
- 272.3
- MOL File
- 396129-53-6.mol
LY-364947 Property
- 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
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
H400Very toxic to aquatic life
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P273Avoid release to the environment.
P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- L6293
- Product name
- LY-364947
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $209
- Updated
- 2024/03/01
- Product number
- 616451-M
- Product name
- TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem
- Packaging
- 616451-5UNMG
- Price
- $18700
- Updated
- 2024/03/01
- Product number
- 616451-M
- Product name
- TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem
- Packaging
- 616451-5MG
- Price
- $189
- Updated
- 2023/06/20
- Product number
- 13341
- Product name
- LY364947
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $92
- Updated
- 2024/03/01
- Product number
- 13341
- Product name
- LY364947
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $174
- Updated
- 2024/03/01
LY-364947 Chemical Properties,Usage,Production
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-364947 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from LY-364947 manufacturers
- Product
- LY-364947 396129-53-6
- Price
- US $0.00-0.00/g
- Min. Order
- 1g
- Purity
- 98%
- Supply Ability
- 1000kgs
- Release date
- 2021-05-24
- Product
- LY-364947 396129-53-6
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 20kg
- Release date
- 2019-09-05