p38 MAPK



  • 阻害剤の選択性比較
  • 溶解度
カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1076 SB203580 <1 mg/mL 43 mg/mL <1 mg/mL
S1574 Doramapimod (BIRB 796) <1 mg/mL 100 mg/mL 100 mg/mL
S1077 SB202190 (FHPI) <1 mg/mL 66 mg/mL 12 mg/mL
S1494 Ralimetinib (LY2228820) 100 mg/mL 4 mg/mL 3 mg/mL
S6005 VX-702 <1 mg/mL 81 mg/mL <1 mg/mL
S8706 UM-164 <1 mg/mL 100 mg/mL <1 mg/mL
S2726 PH-797804 <1 mg/mL 96 mg/mL 7 mg/mL
S1458 VX-745 <1 mg/mL 15 mg/mL <1 mg/mL
S2928 TAK-715 <1 mg/mL 80 mg/mL 16 mg/mL
S8125 Pamapimod (R-1503, Ro4402257) <1 mg/mL 81 mg/mL 28 mg/mL
S7741 SB239063 <1 mg/mL 60 mg/mL 7 mg/mL
S7214 Skepinone-L <1 mg/mL 85 mg/mL 85 mg/mL
S7215 Losmapimod (GW856553X) <1 mg/mL 76 mg/mL 41 mg/mL
S8124 BMS-582949 <1 mg/mL 81 mg/mL <1 mg/mL
S7799 Pexmetinib (ARRY-614) <1 mg/mL 100 mg/mL 100 mg/mL
S2266 Asiatic acid <1 mg/mL 97 mg/mL <1 mg/mL


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SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM.


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.


SB202190 (FHPI)

SB202190 (FHPI) 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.


Ralimetinib (LY2228820)

Ralimetinib (LY2228820) 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.



VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.



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.



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.



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.



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.


Pamapimod (R-1503, Ro4402257)

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.



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.



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


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.



BMS-582949 is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.


Pexmetinib (ARRY-614)

Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.


Asiatic acid

Asiatic acid is the aglycone of asiaticoside isolated from the plant Centella asiatica, commonly used in wound healing.

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