p38 mapk inhibitor

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

(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).

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.

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).

Iroxanadine (BRX-005) is a Novel small molecule MAPK p38 inhibitor that induces phosphorylation of p38 SAPK and induces concentration-dependent relaxation in guinea pig pulmonary artery preparations precontracted with phenylephrine.13480-84-5

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.

Ro-3201195 is a novel orally available p38 MAPK inhibitor with high selectivity.

Scio-323 is an orally available p38 mitogen-activated protein (MAPK) kinase inhibitor.

JNJ-49095397 (RV568) is a selective p38 MAPK-α and p38 MAPK--γ kinase inhibitor with anti-inflammatory activity and potential antiviral activity for chronic obstructive pulmonary disease (COPD), cystic fibrosis, and respiratory syncytial virus infection.

Aspirin is an orally active, selective, and irreversible inhibitor of COX-1 and COX-2 with IC₅₀ values of 5 and 210 μg/mL, respectively. It induces apoptosis, inhibits NF-κB activation and platelet prostaglandin synthesis, thereby preventing thrombosis. Additionally, it acts as a histone deacetylase inhibitor that upregulates p21, exhibiting anti-inflammatory, antipyretic, analgesic, and anti-platelet aggregation activities. Aspirin is commonly used to induce gastric ulcer models.

Oxidopamine hydrobromide (6-OHDA hydrobromide) is a widely used neurotoxin and an antagonist of the neurotransmitter dopamine. It selectively destroys dopaminergic neurons, promotes COX-2 activation, induces PGE2 synthesis, and stimulates the secretion of the pro-inflammatory cytokine IL-1β. It is commonly used to establish animal models of Parkinson’s disease (PD).

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.

Asiatic acid (Dammarolic acid) is the aglycone of asiaticoside used in wound healing with antioxidant, anti-inflammatory, and neuroprotective properties.

Esculin (Aesculin) is a glucoside found in horse chestnuts.

Bakuchiol possesses anti-tumor,and anti-helmenthic properties. It has cytotoxic activity, mainly due to its DNA polymerase1 inhibiting activity. Bakuchiol has anti-bacterial activity against oral pathogens, has great potential for use in food additives and mouthwash for preventing and treating dental caries.

(E)-Ferulic acid methyl ester (Methyl (E)-ferulate) is a potential inhibitor of the mitogen-activated phosphor kinase pathway and an anti-inflammatory agent first isolated from the medicinal plant S. tuberosa. Additionally, it shows promising anthelmintic activity against Haemonchus contortus.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK p38 MAPK signaling pathways in the murine macrophages.