In previous blogs, we have introduced a few MAPK p38 inhibitors. As a result, MAPK p38 plays an important role in many diseases, including cancer and inflammatory diseases. Today, I’d like to mention another MAPK p38α Inhibitor, SD 0006. SD 0006 is a potent diaryl pyrazole inhibitor of p38 MAP kinase.

The mitogen activated protein kinase (MAPK) p38 has been demonstrated to play a critical role in cell signaling pathways which lead to the production of both TNF-a and IL-1B. As a result, p38 represents an attractive candidate for intervention to block biosynthesis of these proinflammatory cytokines. Rheumatoid arthritis (RA) is an autoimmune disease that can cause joint pain and damage throughout your body. The joint damage that RA causes usually happens on both sides of your body. So if a joint is affected in one of your arms or legs, the same joint in the other arm or leg will probably be affected, too. This is one way that doctors distinguish RA from other forms of arthritis, such as osteoarthritis (OA).

A study from John K. Walker firstly discovered and reported SD 0006. The authors described it as a promising clinical candidate to treat rheumatoid arthritis with oral activity.

In animals, SD 0006 possessed desirable properties in terms of half-life with bioavailabilities >80% in both species. On the basis of the data presented, SD 0006 was selected for advancement to clinical trials.

Walker JK, et al. Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2634-8.