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Merck-5
INQ
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)