| S0388 |
SD169 |
SD-169(5-Carbamoylindole) is a selective inhibitor of p38α MAPK, which can reduce p38 and HSP60 expression in T cells of the pancreatic beta islets. |
Selective |
|
| S1574 |
Doramapimod (BIRB 796) |
Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2. |
Selective |
p38α, Kd: 0.1 nM; p38α, IC50: 38 nM |
| S7214 |
Skepinone-L |
Skepinone-L (CBS3830) is a selective p38α-MAPK inhibitor with IC50 of 5 nM. |
Selective |
p38α, IC50: 5 nM |
| S1494 |
Ralimetinib (LY2228820) dimesylate |
Ralimetinib (LY2228820) dimesylate is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, 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 |
| S0542 |
R1487 |
R1487 is an orally bioavailable and highly selective inhibitor of p38α with an ic50 value of 10 nM. |
Selective |
p38α, ic50: 10 nM |
| S1458 |
Neflamapimod (VX-745) |
Neflamapimod (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. |
Selective |
p38α, IC50: 4 nM-20 nM |
| S8125 |
Pamapimod |
Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms. |
Selective |
p38α, IC50: 0.014 μM |
| S6502 |
SD 0006 |
SD0006 is an inhibitor of p38 kinase-alpha (p38alpha) with IC50 values of 0.016 μM and 0.677 μM for p38α and p38β. It is selective for p38α kinase over 50 other kinases screened (including p38γ and p38δ with modest selectivity over p38β). |
Selective |
p38α, IC50: 0.016 μM |
| S7215 |
Losmapimod |
Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. Phase 3. |
Pan |
p38α, pKi: 8.1 |
| S2726 |
PH-797804 |
PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2. |
Pan |
p38α, IC50: 26 nM |
| S7741 |
SB239063 |
SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.
|
Pan |
p38α, IC50: 44 nM |
| S1077 |
SB202190 |
SB202190 is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis. |
Pan |
p38α, IC50: 50 nM |
| S8706 |
UM-164 |
UM-164 is a highly potent, dual c-Src/p38inhibitor of c-Src with a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β. |
Pan |
|
