p38 mapks (P38 mitogen-activated protein kinases) which include p38 isoforms α, β, γ, and δ are a member of mitogen-activated protein kinases family. p38 mapk can be activated by LPS, proinflammatory cytokines, various environmental stresses. p38 MAPK phosphorylates various substrates including MAPK-activated protein kinase 2 (MAPKAPK2). p38 MAPK which is activated in the human brain with Alzheimer’s disease plays more than one role in Alzheimer's disease (AD).
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p38 MAPK inhibitors/activators
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S1076 | SB203580 (Adezmapimod) | Adezmapimod (SB203580, RWJ 64809, PB 203580) 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. SB203580 induces mitophagy and autophagy. |
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| 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. This compound inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. It significantly suppresses Erastin‐dependent ferroptosis. |
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| 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. |
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| S1950 | Metformin Hydrochloride | Metformin Hydrochloride (1,1-Dimethylbiguanide Hydrochloride) is a highly effective Antihyperglycemic Agent, which primarily decreases hyperglycemia in hepatocytes by suppressing hepatic gluconeogenesis (glucose production by the liver). It also promotes mitophagy in mononuclear cells and induces apoptosis of lung cancer cells through activating the JNK/p38 MAPK pathway and GADD153. |
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| 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. It binds p38α with Kd of 0.1 nM in THP-1 cells, showing 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, and insignificant inhibition of ERK-1, SYK, IKK2. |
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| 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. |
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| S6005 | VX-702 | VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. |
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| 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. |
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| 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. |
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| S1458 | Neflamapimod (VX-745) | Neflamapimod (VX-745) is a potent and selective inhibitor of p38α with IC50 of 10 nM, exhibiting 22-fold greater selectivity versus p38β and no inhibition to p38γ. |
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Signaling Pathway Map
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