Extracellular signal regulated kinases

SEW 2871 is an orally available, highly selective S1P1 agonist with an EC50 of 13.8 nM.It reduces the number of lymphocytes in the blood and is used in studies related to diabetes, Alzheimer's disease, liver fibrosis, and inflammation. It activates ERK, Akt and Rac signaling pathways and induces S1P1 internalization and recycling.

Tauroursodeoxycholate (UR 906), also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid that is produced in humans at a low concentration. Tauroursodeoxycholate is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans.Tauroursodeoxycholate is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.

PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.

TBHQ (tert-Butylhydroquinone) is an antioxidant that induces an antioxidant response through the redox-sensitive transcription factor Nrf2.

SCH772984 is an ERK inhibitor that inhibits ERK1 and ERK2 (IC50=4/1 nM) and is highly selective and ATP-competitive. SCH772984 exhibits antitumor activity against BRAF or RAS mutant cells.

Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1 26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).

MK-8353 (SCH900353) is a potent, selective, and orally available inhibitor of ERK1/2 with IC50 values of 23.0 nM and 8.8 nM, respectively.

EF24 (3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone) treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK. EF24 shows potent anti-tumor activity in oral squamous cell carcinoma (OSCC) via deactivation of the MAPK/ERK signaling pathway.

Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx.

Lidocaine Hydrochloride hydrate is an amide local anesthetic, has anti-inflammatory property.

Honokiol (NSC-293100) is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1 ERK2.

1. 2,5-Dihydroxyacetophenone (Quinacetophenone) possess anti-anxiety, and neuroprotective qualities. 2. 2,5-Dihydroxyacetophenone (Quinacetophenone) reatment can induce a sustained activation of JNK, ERK1 2, and p38 MAPKs, it also can potentiate the pro-apoptotic and anti-proliferative effects of bortezomib in U266 cells. 3. 2,5-Dihydroxyacetophenone (Quinacetophenone) has anti-inflammatory activity in activated macrophages, raising the possibility that this compound has a therapeutic potential for inflammatory conditions. 4. 2,5-Dihydroxyacetophenone (Quinacetophenone) is an uncompetitive inhibitor of murine tyrosinase (K(I) 0.28mm), it strongly inhibits both melanogenesis and cellular tyrosinase activity in vitro in 3-isobutyl-1-methylxanthin-stimulated B16 mouse melanoma cells or in vivo in zebrafish and mouse models.

trans-Zeatin ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing.

Ravoxertinib (GDC-0994) is an efficacious, orally available ERK1 2 inhibitor with an IC50 of 1.1 0.3 nM.

Methylthiouracil is a thiourea-class antithyroid agent that inhibits the synthesis of thyroid hormones and is commonly used to treat hyperthyroidism. Studies have shown that Methylthiouracil can also suppress the production of TNF-α and IL-6, as well as inhibit the activation of NF-κB and ERK1/2. It can be used to induce hyperlipidemia and neurological disorder models.

Tizaterkib (AZD-0364) is a potent and selective ERK2 inhibitor.

BAY885 is a new ERK5 inhibitor.

AX-15836 is an inhibitor of ERK5 (IC50 : 8 nM).

CC-90003 is a selective inhibitor of ERK 1/2. It has antitumor activity.

XMD17-109 (ERK5-IN-1) is a new selective ERK-5 inhibitor (EC50: 4.2 uM, HEK293 cells).

XMD8-92 is an effective and specific BMK1 ERK5 inhibitor (Kd: 80 nM).

FR 180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2.

6-OAU (GTPL5846)(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

BIX02189 is a potent and selective inhibitor of MEK5 and ERK5 (IC50: 1.5 nM and 59 nM).