ERK

CK2/ERK8-IN-1 (TMCB) is a dual inhibitor of casein kinase 2 (CK2) (Ki: 0.25 µM) and ERK8 (IC50s: 0.50 μM) with pro-apoptotic efficacy. CK2/ERK8-IN-1 also binds to PIM1, DYRK1A, and HIPK2 (Kis: 8.65 µM, 11.9 µM, and 15.25 µM).

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

ERK5-IN-1 is a potent ERK5 inhibitor (IC50: 87 nM) and also inhibits LRRK2[G2019S] (IC50: 26 nM).

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.

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.

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.

CHPG hydrochloride is a selective agonist of mGluR5.

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.

Olomoucine is an ATP-competitive inhibitor of Cdk2 cyclin A, Cdc2 CyclinB, CDK2 CyclinE, CDK5 p35, and ERK1 p44 MAP kinase with IC50s of 7, 7, 7, 3, and 25 µM, respectively. It regulates the cell cycle and exhibits anti-melanin tumor activities.

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.

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

Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor, and also shows inhibition of CYP1A1 activity.

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.

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.

Tauroursodeoxycholate (TUDCA ,Taurolite) dihydrate is a water-soluble bile acid with endoplasmic reticulum stress inhibitory, mitochondrial stabilizing, and anti-apoptotic effects, which significantly reduces the expression of apoptotic molecules, such as Caspase-3 and Caspase-12, and inhibits ERK, reducing endoplasmic reticulum stress mediated cell death.