Merck-5
| Code | Size | Price |
|---|
| SYN-1054-M100 | 100 mg | Enquire |
Quantity:
| SYN-1054-M050 | 50 mg | Enquire |
Quantity:
| SYN-1054-M001 | 1 mg | £238.00 |
Quantity:
| SYN-1054-M005 | 5 mg | £578.00 |
Quantity:
| SYN-1054-M010 | 10 mg | £824.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
Pyridone 6
Appearance:
Solid.
CAS:
457081-03-7
EClass:
32160000
Form (Short):
liquid
InChi:
InChI=1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)
InChiKey:
VNDWQCSOSCCWIP-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 457081-03-7. Formula: C18H16FN3O. MW: 309.3. 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 .
Molecular Formula:
C18H16FN3O
Molecular Weight:
309.3
Package Type:
Plastic Vial
Product 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 .
Purity:
>95%
Solubility Chemicals:
Soluble in DMSO.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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)
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