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
RWJ-67657
71
CHF
CHF 71.00
In stock
SYN-1072-M0011 mgCHF 71.00
SYN-1072-M0055 mgCHF 106.00
SYN-1072-M01010 mgCHF 142.00
SYN-1072-M05050 mgCHF 546.00
SYN-1072-M100100 mgCHF 937.00
Product Details | |
---|---|
Synonyms | RWJ67657 |
Product Type | Chemical |
Properties | |
Formula | C27H24FN3O |
MW | 425.5 |
CAS | 215303-72-3 |
Purity Chemicals | ≥95% |
Appearance | Solid. |
Solubility | Soluble in DMSO or ethanol. |
Declaration | Manufactured by SynKinase. |
Other Product Data |
Target: p38 | Kinase Group: CMGC | Substrate: Serine-Threonine Click here for Original Manufacturer Product Datasheet Our product description may differ slightly from the original manufacturers product datasheet. |
InChi Key | QSUSKMBNZQHHPA-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
The cytokine Tumor necrosis factor-α (TNF-α) is secreted by activated monocytes/macrophages and T lymphocytes and has been implicated in several disease states, including rheumatoid arthritis, inflammatory bowel disease, septic shock, and osteoporosis. Monocyte/macrophage production of TNF-α is dependent on the mitogen-activated protein kinase p38. The compound RWJ 67657 is a potent, orally active inhibitor of MAPK and it inhibited the release of TNF-α from LPA stimulated human mononuclear cells with an IC(50) of 3nM, as well as the release of TNF-α from peripheral blood mononuclear cells treated with the T cell stimulator and superantigen staphylococcal enterotoxin B with an IC(50) value of 13nM. Also RWJ 67657 was approximately 10-fold more potent than the literature standard p38 kinase inhibitor SB 203580 in all p38 dependent in vitro systems tested and is much more specific than SB 203580 for p38 kinaes. RWJ 67657 inhibited the enzymatic activity of recombinant p38α and β, with in vitro IC(50) values of 1 and 11µM respectively, but not γ or δ, and in further in vitro test across a panel of other enzymes RWJ 67657 demonstrated no other significant activity.
Product References
- RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase: S.A. Wadsworth, et al.; J. Pharmacol. Exp. Ther. 291, 680 (1999)
- Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection: S. Wei, et al.; Antimicrob. Agents Chemother. 51, 4324 (2007)