p38 MAPK

p38 MAPK inhibitor is a potent inhibitor of p38 MAP kinase (IC50 = 35 nM). It inhibits senescence induced by the oncogene RAS.

p38 MAPK-IN-2 is a potent inhibitor of p38 kinase.

p38 MAPK-IN-1 is a novel selective p38 MAPK inhibitor with high potency, long duration, and low clearance, which reduces inflammatory responses by inhibiting LPS-induced TNF-α production.

p38 MAPK-IN-6 (compound c47) is an inhibitor of p38 MAPK, exhibiting a 14% inhibition rate at a concentration of 10 μM.

p38 MAPK-IN-8 (Compound 8) is an orally active, potent, and selective inhibitor of p38 mitogen-activated protein kinase (p38 MAPK). It holds potential for research in inflammatory responses, autoimmune diseases, and cancer.

p38 MAPK-IN-7 (Compound 2) is an orally active and potent inhibitor of p38 MAP kinase, with an IC50 of 170 nM. It holds potential in the study of inflammatory diseases, including rheumatoid arthritis and septic shock.

p38 MAPK-IN-10 (Compound 4) is an orally active and potent inhibitor of p38 MAP kinase, with an IC50 of 570 nM. It shows promise for research into chronic inflammatory diseases, including rheumatoid arthritis and Crohn's disease.

p38 MAPK-IN-9 (Compound 15) is an orally active and highly selective inhibitor of the p38αMAP kinase (p38 MAPK), with an IC50 value of 9.6 nM. It holds potential for research into inflammatory diseases such as rheumatoid arthritis, septic shock, and chronic obstructive pulmonary disease.

(S)-p38 MAPK inhibitor III is a methylsulfanylimidazole that inhibits p38 MAP kinase (IC50 = 0.90 μM in vitro). It is cell-permeable, potently blocking the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC50s = 0.37 and 0.044 μM, respectively).

p38 MAPK-IN-3 (Compound 2c) is a potent inhibitor of p38α MAPK, exhibiting antitumor properties through the promotion of apoptosis and the enhancement of reactive oxygen species (ROS) production [1].

p38 MAPK inhibitor IV is an ATP-competitive inhibitor of p38 MAP kinases with IC50 values of 0.13, 0.55, 5.47, and 8.63 μM for p38α, p38β, p38x, and p38δ, respectively, in vitro.[1] It also inhibits LPS-induced TNF-α and IL-1β cytokine production (IC50s = 22 and 44 nM, respectively) in human peripheral blood mononuclear cells.

p38αMAPK/CK1δ inhibitor-1 (Compound 3) exhibits inhibitory activity against p38αMAPK and CK1δ, with IC50 values of 0.185 µM and 0.089 µM, respectively.

Adezmapimod (SB 203580) is a selective, ATP-competitive p38 MAPK inhibitor (IC50=0.3-0.5 μM) that activates autophagy and mitochondrial autophagy, with more than 100-fold higher selectivity over PKB, LCK, and GSK-3β.

SB 202190 (FHPI) is a p38 MAPK inhibitor that inhibits p38α and p38β2 (IC50=50/100 nM) selectively and cell-permeably. SB 202190 has antitumor activity and also induces the differentiation of human embryonic stem cells into cardiomyocytes.

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug/mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.

Doramapimod (BIRB 796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.

PAF (C16) is a potent MAPK and MEK/ERK activator that induces increased vascular permeability. PAF (C16) (PAF (C16)) is a platelet-activating factor, a phospholipid-derived mediator and a ligand for PAF G protein-coupled receptor (PAFR). PAF (C16) has shown anti-apoptotic and anti-inflammatory activity in vitro, inhibiting Caspase-dependent apoptosis by interacting with its receptor (PAF-R) to perform cell signaling.

Darizmetinib (HRX215, HRX-0215) is an MKK4 inhibitor. Inhibition of MKK4 leads to enhancement of the MKK7 and JNK1 signaling pathways, thereby activating the transcription factors ATF2 and ELK1, promoting cell proliferation and liver regeneration.

AL 8697 is a selective p38α MAPK inhibitor (IC50 = 6 nM) with 14-fold selectivity over p38β (IC50 = 82 nM) and 300-fold selectivity over a panel of 91 kinases. AL 8697 has anti-inflammatory activity.

Talmapimod (SCIO-469) is a selective, orally active, ATP-competitive p38α inhibitor with IC50 values of 9 nM for p38α and 90 nM for p38β. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.

SR-318 is a potent and highly selective inhibitor of p38 MAPK, demonstrating IC50 values of 5 nM for p38α, 32 nM for p38β, and 6.11 μM for p38α/β. It possesses both anti-cancer and anti-inflammatory activity.

VX-702 is a highly specific p38α MAPK inhibitor, 14-fold higher selectivity for the p38α than p38β. VX-702 is a small molecule investigational oral anti-cytokine therapy for treatment of inflammatory diseases, specifically rheumatoid arthritis (RA).

UR-13870 (Org 48762-0) is an orally active and selective inhibitor of p38 mitogen-activated protein kinase (MAPK), which prevents bone damage in collagen-induced arthritis in mice.

EO-1606 is a p38MAP kinase inhibitor with anti-inflammatory activity and may be used in studies of Alzheimer;s disease and dermatitis.