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. |
C57BL/6 male mice (8 weeks, Harlan) were pretreated with by intravenous injections with PERY or SCR peptides (15 mg/kg) or DMSO. The following day, mice were treated with 1.5% dextran sodium sulfate (DSS) in drinking water for 7 days followed by 3 days of normal drinking water. During DSS administration, mice were treated every other day (total of five intravenous injections). Control groups included nontreated mice (no DSS, no treatment) and mice receiving PERY peptide with normal drinking water (PERY only, no DSS). Mice were then euthanized and analyzed. Colitis was evaluated using (C) hematoxylin and eosin (H&E) histological sections of the colons (top) and their magnifications (bottom). Scale bar, 2 mm.
|
|
| 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. |
Lympho-myeloid potential assessed by FACS analysis of human CD19 (B-lymphoid cells) and CD33/CD15 (myeloid cells) in bone marrow of NSG recipient mice, 17 weeks after transplantation. Each plot represents an animal from the experiment presented in panel.
|
|
| 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. |
CD34 expression after 14 days of culture of CB CB CD34+ cells treated with the P38α inhibitor Ly2228820 or vehicle (DMSO; n=3). Error bars represent SEM.
|
|
| S6005 |
VX-702VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2. |
|
|
| S8706New |
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. |
||
| 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. |
Human perforated disk cells were pretreated with specific pathway inhibitors, BAY11-7082 (NF-jF inhibitor) and PH797804 (p38 inhibitor), atdifferent concentrations (1, 10 ng/ml) for 1 h and then incubated with IL-1b for 48 h. (B) VEGFAexpression was quantified and analyzed; (C) Ang-1 expression; (D) TSP-1 expression; (E) ChM-1 expression. Expression levels were uniformly set to a valueof 1 in PBS group. Data are presented as mean±SEM (n = 3) and analyzed by one-way ANOVA test. *P < 0.05 as compared with IL-1b-induced group.
|
|
| 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 |
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. |
||
| 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. |
||
| 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. |
C57BL/6 male mice (8 weeks, Harlan) were pretreated with by intravenous injections with PERY or SCR peptides (15 mg/kg) or DMSO. The following day, mice were treated with 1.5% dextran sodium sulfate (DSS) in drinking water for 7 days followed by 3 days of normal drinking water. During DSS administration, mice were treated every other day (total of five intravenous injections). Control groups included nontreated mice (no DSS, no treatment) and mice receiving PERY peptide with normal drinking water (PERY only, no DSS). Mice were then euthanized and analyzed. Colitis was evaluated using (C) hematoxylin and eosin (H&E) histological sections of the colons (top) and their magnifications (bottom). Scale bar, 2 mm.
|
|
| 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. |
Lympho-myeloid potential assessed by FACS analysis of human CD19 (B-lymphoid cells) and CD33/CD15 (myeloid cells) in bone marrow of NSG recipient mice, 17 weeks after transplantation. Each plot represents an animal from the experiment presented in panel.
|
|
| 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. |
CD34 expression after 14 days of culture of CB CB CD34+ cells treated with the P38α inhibitor Ly2228820 or vehicle (DMSO; n=3). Error bars represent SEM.
|
|
| S6005 |
VX-702VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2. |
|
|
| S8706New |
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. |
||
| 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. |
Human perforated disk cells were pretreated with specific pathway inhibitors, BAY11-7082 (NF-jF inhibitor) and PH797804 (p38 inhibitor), atdifferent concentrations (1, 10 ng/ml) for 1 h and then incubated with IL-1b for 48 h. (B) VEGFAexpression was quantified and analyzed; (C) Ang-1 expression; (D) TSP-1 expression; (E) ChM-1 expression. Expression levels were uniformly set to a valueof 1 in PBS group. Data are presented as mean±SEM (n = 3) and analyzed by one-way ANOVA test. *P < 0.05 as compared with IL-1b-induced group.
|
|
| 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 |
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. |
||
| 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. |
| 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. |
