Merck-5

CHF 233.00
In stock
SYN-1054-M0011 mgCHF 233.00
SYN-1054-M0055 mgCHF 581.00
SYN-1054-M01010 mgCHF 832.00
SYN-1054-M05050 mgCHF 2'370.00
SYN-1054-M100100 mgCHF 3'818.00
 
More Information
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
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
  1. Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor: J.E. Thompson, et al.; Bioorg. Med. Chem. Lett. 12, 1219 (2002)
  2. A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases: O. Fedorov, et al.; PNAS 104, 20523 (2007)
  3. 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)
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