BCC8037
AL 8697
AL 8697, a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM, 14-fold less potent in p38β MAPK (IC50=82 nM), exhibits anti-inflammatory activity.
BCC1953
Skepinone-L
Skepinone-L (CBS3830) is a selective p38 mitogen-activated protein kinase inhibitor.
BCC1093
SB202190 (FHPI)
SB 202190 is a cell-permeable p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM.
BCC3663
SB 203580
SB 203580 (RWJ 64809) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 does not disrupt JNK activity and is an autophagy and mitophagy activator.
BCC3969
PD 169316
PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor, with IC50 of 89 nM. PD169316 selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. PD169316 shows antiviral activity against Enterovirus71. PD169316 shows antiviral activity against Enterovirus71.
BCC1923
SB 239063
SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD.
BCC4171
SB 242235
SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0 μM in primary human chondrocytes.
BCC3966
VX-745
Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
BCC1937
SD-06
SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP kinase, with an IC50 of 110 nM for p38α.
BCC2535
BIRB 796 (Doramapimod)
Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod (BIRB 796) has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod (BIRB 796) also inhibits B-Raf with an IC50 of 83 nM.
BCC3968
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.
BCC7274
CMPD-1
CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Kiapp) of 330 nM.
BCC5368
Losmapimod
Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.
BCC3672
PH-797804
PH-797804 is a ATP-competitive, selective p38α/p38β inhibitor (IC50=26 nM and Ki=5.8 nM for p38α; Ki=40 nM for p38β) and does not inhibit JNK2.
BCC2528
LY2228820
Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
BCC6084
AMG 548
AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
BCC4293
SB 203580 hydrochloride
SB 203580 hydrochloride (RWJ 64809 hydrochloride) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 hydrochloride is an autophagy and mitophagy activator.
BCC6509
Pexmetinib (ARRY-614)
Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
