Cookie Policy: This site uses cookies to improve your experience. You can find out more about our use of cookies in our Privacy Policy. By continuing to browse this site you agree to our use of cookies.
SynKinase
Merck-5
CHF 0.00
In stock
SYN-1054-M0011 mgCHF 277.00
SYN-1054-M0055 mgCHF 688.00
SYN-1054-M01010 mgCHF 986.00
SYN-1054-M05050 mgINQ
SYN-1054-M100100 mgINQ
| Product Details | |
|---|---|
| Synonyms | Pyridone 6 |
| Product Type | Chemical |
| Properties | |
| Formula | C18H16FN3O |
| MW | 309.3 |
| CAS | 457081-03-7 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data |
Target: JAK | Kinase Group: PTK | Substrate: Tyrosine Click here for Original Manufacturer Product Datasheet Our product description may differ slightly from the original manufacturers product datasheet. |
| InChi Key | VNDWQCSOSCCWIP-UHFFFAOYSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
Merck 5, also known as Pyridone 6, is a potent and reversible ATP-competitive inhibitor of the JAK kinases (JAK1, JAK2, JAK3, and Tyk2) with IC(50) values in the low anomolar range. At higher values (IC(50) >100nM) Merck 5 also can inhibit ERK kinase family and appear to block IL-2 and IL-4 dependent proliferation of CTLL cells and inhibits the phosphorylation of STAT5. In research comparing Merck 5 (Pyridone 6) to the Jak inhibitor AG490, Merck 5 demonstrated much lower effective drug concentrations and faster kinetics and appear to be a more sensitive and specific inhibitor of JAK-STAT3 activity compared with AG490 and potently inhibited the growth of primary myeloma cells and myeloma-derived cell lines grown on bone marrow-derived stromal cells .
Product References
- Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor: J.E. Thompson, et al.; Bioorg. Med. Chem. Lett. 12, 1219 (2002)
- A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases: O. Fedorov, et al.; PNAS 104, 20523 (2007)
- Virtual screening to successfully identify novel janus kinase 3 inhibitors: a sequential focused screening approach: X. Chen, et al.; J. Med. Chem. 51, 7015 (2008)