sb-203580

SB 203580 sulfone, an analog of the p38 MAP kinase inhibitor SB 203580, inhibits IL-1 production in monocytes and binds competitively with CSAID binding proteins (CSBP), inhibiting stress response signaling. It exhibits an IC50 of 0.2 μM for IL-1 inhibition and 0.03 μM for CSBP-mediated signaling inhibition [1].

Adezmapimod (SB 203580) hydrochloride is a selective ATP-competitive inhibitor of p38 MAPK, with IC50 values of 50 nM for SAPK2a p38 and 500 nM for SAPK2b p38β2. This compound also inhibits LCK, GSK3β, and PKBα with IC50 values 100-500 times higher than those for SAPK2a p38. Additionally, Adezmapimod hydrochloride acts as an activator of autophagy and mitophagy [1].

Adezmapimod (SB 203580) is a selective, ATP-competitive p38 MAPK inhibitor (IC50=0.3-0.5 μM) that activates autophagy and mitochondrial autophagy, with more than 100-fold higher selectivity over PKB, LCK, and GSK-3β.

Tie2 kinase inhibitor 1 (Tie2 kinase inhibitor), an optimized compound of SB-203580, is selective to Tie2 with IC50 of 0.25 μM, which is 200-fold more effective than p38.