p38α Selective Inhibitors
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
|S1574||BIRB 796 (Doramapimod)||
BIRB 796 (Doramapimod) is a highly selective p38α MAPK inhibitor with Kd of 0.1 nM, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2, ZAP-70, EGFR, HER2, PKA, PKC, PKCα/β/γ.
|Selective||p38α, Kd: 0.1 nM|
Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM.
|Selective||p38α, IC50: 5 nM|
LY2228820 is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM, does not alter p38 MAPK activation. Phase 1/2.
|Selective||p38α, IC50: 7 nM|
TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.
|Selective||p38α, IC50: 7.1 nM|
VX-745 is a potent and selective inhibitor of p38α with IC50 of 10 nM, 22-fold greater selectivity versus p38β and no inhibition to p38γ.
|Selective||p38α, IC50: 10 nM|
VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.
|Selective||p38α, IC50: 4 nM-20 nM|
Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.
|Pan||p38α, pKi: 8.1|
PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.
|Pan||p38α, IC50: 26 nM|
SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo.
|Pan||p38α, IC50: 50 nM|
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