p38 MAPK
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Isoform-specific Inhibitors
p38 MAPK Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1076 |
SB203580SB203580 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. |
A, effects of p38 inhibitor SB203580 (1, 5, and 10 μM) on SRP72 protein expression was evaluated by WB using antibodies against human SRP72,SRP54, and GAPDH. A decreased intensity of SRP72 bands was noted when using the inhibitor at 5 μM concentration at 240 min (lane 6) and 10 μM at 120 and 240 min (lanes 8 and 9). B, results were analyzed and RUA illustrated, finding significant results at 5 μM, 240 versus 0 min, and 10 μM, 240 versus 0 and 120 versus 0 min, respectively, (p<0.05).
|
|
| 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. |
Effect of blockade of p38 or MEK on MK2 activation following TLR stimulation in moDC. MoDC were pre-treated with p38 inhibitors SB203580 10 mM (S), BIRB0796 (B) 0.1 or 1.0 mM or MEK inhibitor UO126 10 mM (U) for 1hr followed by poly I:C/R848 stimulation for 30 min then Western blotted for p-MK2 with β-actin loading control.
|
|
| S1077 |
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. |
C, Jurkat cells with SB202190 at 1, 5, and 10 μM were tested, and a decreased SRP72 expression was found when using at 10 μM (lanes 8 and 9). D, results were analyzed and RUA illustrated, finding significant results at 10 μM at 240 versus 0 and 120 versus 0 min (p<0.05).
|
|
| S1494 |
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. |
Relationship of JNK, p38 MAPK, and PI3K activation in TNF-α-induced signaling. Western blot analysis of the effect of another p38 MAPK inhibitor, LY2228820, on TNF-α signaling. HUVECs were pretreated with LY2228820 (10 umol/L) or wortmannin (1 umol/L) for 1 h, followed by stimulation with TNF-α (5 ng/mL) for 15 min (n=2).
|
|
| S6005 |
VX-702VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2. |
Reduction of IL-10 expression due to p38 inhibition is observed also in CpG-stimulated B cells and using VX-702. B cells were pre-treated with 10 uM of VX-702 for 1 h and stimulated with LPS or CpG for 24 or 48 h. Bar graphs indicate mean (±SEM) IL-10 concentrations at 48 h from n = 4 (LPS) and n = 3 (CpG) experiments. Significant differences against the no inhibitor condition were calculated using a paired Student's t-test and indicated as follows: *p < 0.05, ***p < 0.001. |
|
| S8734New |
AZD7624AZD7624 is a potent and selective competitive inhibitor against p38α/β with pIC50s of 10 and 8.8 for p38α and p38β respectively. |
||
| S6502New |
SD 0006SD0006 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). |
||
| S2726 |
PH-797804PH-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. |
Effect of MEK inhibitor PH-797804 in A549 cells. A549 cells were incubated with increasing concentrations of PH-797804 for 2 h. The cell lysates were harvested and phosphorylation of indicated proteins was determined by Western blotting.
|
|
| S1458 |
VX-745VX-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. |
A) TRAP staining of BMMs cultured with M-CSF and RANKL for 7 d in the presence of SB203580 (50 nM) or VX-745 (50 nM). B) Bone slice assay indicated the effects of compounds on bone resorption.
|
|
| S2928 |
TAK-715TAK-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. |
||
| S8125 |
PamapimodPamapimod (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. |
||
| S7741 |
SB239063SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms. |
KLF4 protein half-life is elongated under p38 inhibition. MCF7 cells plated in six-well plate were treated with DMSO or p38 inhibitors (SB203580 and SB239063) for 6 h. Then CHX was added 0, 2, 4 or 6 h before harvest. KLF4 protein level was tested by immunoblotting |
|
| S7214 |
Skepinone-LSkepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM. |
TLR4/MAPK pathway regulated macrophage polarization towards M1 phenotype. LPS/INF-γ induced macrophages were cultured in the absence or presence of siTLR4, SP600125(an inhibitor of JNK), SCH772984(an inhibitor of ERK) and Skepinone-L(an inhibitor of p38) respectively for 24h. Then, all the cells were harvested for western blot assay.
|
|
| 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. |
Intracellular pathways of b-adrenoceptor-induced proliferation. Urothelial proliferation (% of basal responses) in T24 in the absence and presence of (d) losmapimod (1-30 μM).
|
|
| S8124 |
BMS-582949BMS-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. |
||
| S7799 |
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. |
||
| S8706 |
UM-164UM-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. |
||
| S2266 |
Asiatic AcidAsiatic acid is the aglycone of asiaticoside isolated from the plant Centella asiatica, commonly used in wound healing. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1076 |
SB203580SB203580 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. |
A, effects of p38 inhibitor SB203580 (1, 5, and 10 μM) on SRP72 protein expression was evaluated by WB using antibodies against human SRP72,SRP54, and GAPDH. A decreased intensity of SRP72 bands was noted when using the inhibitor at 5 μM concentration at 240 min (lane 6) and 10 μM at 120 and 240 min (lanes 8 and 9). B, results were analyzed and RUA illustrated, finding significant results at 5 μM, 240 versus 0 min, and 10 μM, 240 versus 0 and 120 versus 0 min, respectively, (p<0.05).
|
|
| 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. |
Effect of blockade of p38 or MEK on MK2 activation following TLR stimulation in moDC. MoDC were pre-treated with p38 inhibitors SB203580 10 mM (S), BIRB0796 (B) 0.1 or 1.0 mM or MEK inhibitor UO126 10 mM (U) for 1hr followed by poly I:C/R848 stimulation for 30 min then Western blotted for p-MK2 with β-actin loading control.
|
|
| S1077 |
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. |
C, Jurkat cells with SB202190 at 1, 5, and 10 μM were tested, and a decreased SRP72 expression was found when using at 10 μM (lanes 8 and 9). D, results were analyzed and RUA illustrated, finding significant results at 10 μM at 240 versus 0 and 120 versus 0 min (p<0.05).
|
|
| S1494 |
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. |
Relationship of JNK, p38 MAPK, and PI3K activation in TNF-α-induced signaling. Western blot analysis of the effect of another p38 MAPK inhibitor, LY2228820, on TNF-α signaling. HUVECs were pretreated with LY2228820 (10 umol/L) or wortmannin (1 umol/L) for 1 h, followed by stimulation with TNF-α (5 ng/mL) for 15 min (n=2).
|
|
| S6005 |
VX-702VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2. |
Reduction of IL-10 expression due to p38 inhibition is observed also in CpG-stimulated B cells and using VX-702. B cells were pre-treated with 10 uM of VX-702 for 1 h and stimulated with LPS or CpG for 24 or 48 h. Bar graphs indicate mean (±SEM) IL-10 concentrations at 48 h from n = 4 (LPS) and n = 3 (CpG) experiments. Significant differences against the no inhibitor condition were calculated using a paired Student's t-test and indicated as follows: *p < 0.05, ***p < 0.001. |
|
| S8734New |
AZD7624AZD7624 is a potent and selective competitive inhibitor against p38α/β with pIC50s of 10 and 8.8 for p38α and p38β respectively. |
||
| S6502New |
SD 0006SD0006 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). |
||
| S2726 |
PH-797804PH-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. |
Effect of MEK inhibitor PH-797804 in A549 cells. A549 cells were incubated with increasing concentrations of PH-797804 for 2 h. The cell lysates were harvested and phosphorylation of indicated proteins was determined by Western blotting.
|
|
| S1458 |
VX-745VX-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. |
A) TRAP staining of BMMs cultured with M-CSF and RANKL for 7 d in the presence of SB203580 (50 nM) or VX-745 (50 nM). B) Bone slice assay indicated the effects of compounds on bone resorption.
|
|
| S2928 |
TAK-715TAK-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. |
||
| S8125 |
PamapimodPamapimod (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. |
||
| S7741 |
SB239063SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms. |
KLF4 protein half-life is elongated under p38 inhibition. MCF7 cells plated in six-well plate were treated with DMSO or p38 inhibitors (SB203580 and SB239063) for 6 h. Then CHX was added 0, 2, 4 or 6 h before harvest. KLF4 protein level was tested by immunoblotting |
|
| S7214 |
Skepinone-LSkepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM. |
TLR4/MAPK pathway regulated macrophage polarization towards M1 phenotype. LPS/INF-γ induced macrophages were cultured in the absence or presence of siTLR4, SP600125(an inhibitor of JNK), SCH772984(an inhibitor of ERK) and Skepinone-L(an inhibitor of p38) respectively for 24h. Then, all the cells were harvested for western blot assay.
|
|
| 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. |
Intracellular pathways of b-adrenoceptor-induced proliferation. Urothelial proliferation (% of basal responses) in T24 in the absence and presence of (d) losmapimod (1-30 μM).
|
|
| S8124 |
BMS-582949BMS-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. |
||
| S7799 |
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. |
||
| S8706 |
UM-164UM-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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2266 |
Asiatic AcidAsiatic acid is the aglycone of asiaticoside isolated from the plant Centella asiatica, commonly used in wound healing. |
