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Published TCIMAIL newest issue No.201
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CAS RN: 220904-83-6 | Product Number: G0609
GW-5074
Purity: >95.0%(HPLC)
Synonyms:
- 3-(3,5-Dibromo-4-hydroxybenzylidene)-5-iodoindolin-2-one
Product Documents:
* Stock available in Belgium: Shipment on the same day
* Stock available in Japan: Please check the Shipping Simulation for estimated shipments. (excludes regulated items and dry ice shipments)
| Product Number | G0609 |
Purity / Analysis Method
|
>95.0%(HPLC) |
| Molecular Formula / Molecular Weight | C__1__5H__8Br__2INO__2 = 520.95 |
| Physical State (20 deg.C) | Solid |
Storage Temperature
|
Room Temperature (Recommended in a cool and dark place, <15°C) |
| Store Under Inert Gas | Store under inert gas |
| Condition to Avoid | Light Sensitive,Air Sensitive |
Packaging and Container
|
100MG-Glass Bottle with Plastic Insert (View image) |
| CAS RN | 220904-83-6 |
| Reaxys Registry Number | 8641129 |
| MDL Number | MFCD09971042 |
Specifications
| Appearance | White to Yellow powder to crystal |
| Purity(HPLC) | min. 95.0 %(total of isomers) |
| NMR | confirm to structure |
Properties (reference)
| Melting Point | 262 °C |
GHS
Related Laws:
| RTECS# | NM3249100 |
Transport Information:
| HS Number | 2933790090 |
Application
GW5074: An Inhibitor of Raf-1 and LRRK2
GW5074 has been used as a potent and selective inhibitor of Raf-1 (c-Raf) which is a serine/threonine protein kinase that signals from Ras to the MAPK/ERK signaling pathway.1,2) Recently, it has been reported that GW5974 is also an inhibitor of the autophosphorylation of leucine-rich repeat kinase 2 (LRRK2), which is a large, multidomain protein containing two catalytic domains: a Ras of complex proteins (Roc) G-domain and a kinase domain.3-6) GW5074 is of interest for studying Parkinson's disease (PD), because mutations in the gene encoding Parkinson’s protein LRRK2 indicate LRRK2 as promising therapeutic target for the treatment of PD. (The product is for research purpose only.)
References
- 1) The discovery of potent cRaf1 kinase inhibitors
- 2) Untying the regulation of the Raf-1 kinase (a review)
- 3) Structural model of the dimeric Parkinson’s protein LRRK2 reveals a compact architecture involving distant interdomain contacts
- 4) Inhibitors of LRRK2 kinase attenuate neurodegeneration and Parkinson-like phenotypes in Caenorhabditis elegans and Drosophila Parkinson's disease models
- 5) LRRK2 G2019S mutation attenuates microglial motility by inhibiting focal adhesion kinase
- 6) Development of LRRK2 Inhibitors for the Treatment of Parkinson's Disease (a review)
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