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
S7214 Skepinone-L

Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM.

Selective p38α, IC50: 5 nM
S1494 LY2228820

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
S2928 TAK-715

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
S1458 VX-745

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
S6005 VX-702

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
S7215 Losmapimod (GW856553X)

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
S2726 PH-797804

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
S1077 SB202190 (FHPI)

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