ERK

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.

Gardenin A shows neurotrophic effects via activating MAPK ERK, PKC, and PKA. Gardenin A exhibits antidepressant, anticonvulsant and anxiolytic effects.

Beta-Tocopherol has effects on human erythroleukemia cell (HEL) adhesion induced by phorbol 12-myristate 13-acetate (PMA).

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.

Notoginsenoside R1 (Sanchinoside R1) has been shown to exhibit antioxidant, antiapoptotic, anti-inflammatory, and immune-stimulatory properties.

Temuterkib (LY3214996) is a potent and selective, orally available inhibitor of the extracellular signal-regulated kinase (ERK) 1 and 2, with potential antineoplastic activity.

Methylnissolin is a natural product isolated from Astragalus membranaceus that inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. It inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibiting the ERK1 2 MAP kinase cascade. It also inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1 2 (ERIC1 2) mitogen-activated protein (MAP) kinases and has antibacterial and anticancer effects.

Ulixertinib (VRT752271) (BVD-523, VRT752271) is an effective and reversible ERK1 ERK2 inhibitor. The IC50 of Ulixertinib is less than 0.3 nM for ERK2.

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.

ERK-IN-3 (ASN007 free base) is a potent and orally active inhibitor of ERK. It inhibits ERK1 2 with low single-digit nM IC50 values. It can be used for the research of cancers driven by RAS mutations.

mSIRK (G-Protein βγ Binding Peptide) is a cell-permeable activator of ERK 1 2 with an EC50 of 2.5-5 μM. It disrupts the interaction between the α and βγ subunits, facilitating α subunit dissociation without inducing nucleotide exchange [1].

Licochalcone D may be a potential drug for human melanoma treatment by inhibiting proliferation, inducing apoptosis via the mitochondrial pathway and blocking cell migration and invasion. Licochalcone D has cardioprotective potential against myocardial is

Nothofagin has antioxidant, and antithrombotic activities, it possesses anti-inflammatory activity by inhibiting hyperpermeability, expression of CAMs, and adhesion and migration of leukocytes, thereby endorsing its usefulness as a therapy for vascular inflammatory diseases.

Selumetinib (AZD6244) is a MEK1 2 inhibitor that inhibits MEK1 (IC50=14 nM) with potent selectivity and is non-ATP-competitive. Selumetinib has antitumor activity and is used for the treatment of neurofibromatosis type 1 (NF1).

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

AY 77 (Unk-Cha-Chg-NH2) is a potent and selective PAR2 agonist. AY 77 showed selectivity for Ca2+ and ERK1 2 signaling (ec50 value of Ca2+ release was 40 nM and ec50 value of ERK1 2 phosphorylation was 2 μM). AY 77 can promote migration of human breast cancer cells in vitro.

12(S)-HETE, a 12-lipoxygenase metabolite of arachidonic acid, is mitogenic for cancer cell proliferation and enhances angiotensin II-induced contraction of BLT2 (type 2 receptor in arteries of leukotriene B4 mice) and TP (thromboxane receptor)-mediated mechanisms. 12(S)-HETE promotes superoxide and isothromboxane-like metabolites in arterial endothelial cells. production.

Chrysoeriol has antioxidant, antiinflammatory, antitumor, antimicrobial, antiviral, and free radical scavenging activities, it also shows selective bronchodilator effect.

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

Sulforaphene is a natural product isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10 -4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1 2, NF‐κB and other signa

Tenuifoliside A has anti-apoptotic , neuroprotective activity. And tenuifoliside A has anti-inflammatory effect, which is mediated by the inhibition of the NF-κB and MAPK pathways.

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.

Vincristine binds to tubulin and inhibits the formation of microtubules, thereby inhibiting mitosis of the cancer cell. Vincristine can be used as a microtubule-destabilizing agent for research on the treatment of hematologic cancers, such as leukemia and

Prosaptide TX14(A) acetate is a potent GPR37L1 and GPR37 agonist. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells.

Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.

Patritumab (U3-1287) is an anti-HER3 monoclonal antibody with potential antitumor activity and inhibits phosphorylation of EGFR, HER2, HER3, ERK, and AKT.Patritumab promotes apoptosis and inhibits proliferation in non-small cell lung cancer.

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

Gypenoside L inhibits autophagic flux and induces cell death in human esophageal cancer cells through endoplasm reticulum stress-mediated Ca2+ release. It also inhibit non-small cell lung carcinoma A549 cell inhibitory activity.

Astragaloside IV (AS-IV), an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1 2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts.

Pachymic acid (3-O-Acetyltumulosic acid) is a natural product, and inhibits Akt and ERK signaling pathways.

Pluripotin (SC1) (SC1), which keep embryonic stem cell (ESC) self-renewal, is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP.

Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.

1. Cornuside (Comuside) has immunomodulatory activity . 2. Cornuside suppresses expression levels of cytokine-induced proinflammatory and adhesion molecules in the human endothelial cells. 3. Cornuside can treat myocardial I R and protect the liver from CCl4-induced acute hepatotoxicity, by reducing oxidative stress and suppressing inflammatory responses. 4. Cornuside has anti-inflammatory activity by downregulations of iNOS and COX-2 due to NF-κB inhibition as well as the negative regulation of ERK1 2, p38, and JNK1 2 phosphorylations in RAW 264.7 cells. 5. Cornuside has protective potential against cerebral ischemic injury, may be due to the suppression of intracellular Ca(2+) elevation and caspase-3 activity, and improvements in mitochondrial energy metabolism and antioxidant properties.

1. Prunetin (Prunusetin) significantly reduces serum levels of inflammatory cytokines and mortality in mice challenged with lipopolysaccharide. 2. Prunetin mediates anti-obesity adipogenesis effects by suppressing obesity-related transcription through a feedback mechanism that regulates the expression of adiponectin, adipoR1, adipoR2, and AMPK. 3. Prunetin and biochanin A are potent reducers of NF-κB and ERK activation, zonula occludens 1 tyrosine phosphorylation, and metalloproteinase-mediated shedding activity, which may account for the barrier-improving ability of these isoflavones. 4. Prunetin significantly suppresses ATP-induced mucin secretion from cultured RTSE cells; Prunetin inhibits the production of MUC5AC mucin protein induced by EGF or PMA from NCI-H292 cells; Prunetin also inhibits the expression of MUC5AC mucin gene induced by EGF or PMA from NCI-H292 cells.

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

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

Piperlongumine (Piplartine) is a natural alkaloid from Piper longum L. It selectively kills cancer cells and strengthens the level of reactive oxygen species (ROS).

A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).

ERK1 2 inhibitor 2 (ASTX029) is a selective and orally bioavailable extracellular signal-regulated kinases 1 and 2 (ERK 1 2) inhibitor, with potential antineoplastic activity.

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50 values of 0.82 μM for ERK5 and 3 μM for ERK5 (MEF2D).

ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, exhibiting an EC50 value of 0.3 nM for ERα degradation. It can be used for the prevention and treatment of HER-positive breast cancer.

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.

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.

Dehydroeffusol (Dehydro Effusol) possesses anti-cancer, anxiolytic and sedative properties. Dehydroeffusol inhibits gastric cancer cell growth and tumorigenicity by selectively inducing tumor-suppressive endoplasmic reticulum stress and a moderate apoptosis.

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

1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf MEK1 ERK1 2 and AMPKα Akt pathways during 3T3-L1 adipocyte differentiation. 3. Epiberberine, as the brightest FSA emitter among the alkaloids, can also serve as an efficient conformation probe for HTG DNA and discriminate the DNA G-quadruplex from the RNA counterpart.

Hederacolchiside A1 (Raddeanoside R13) shows anti-leishmanial activity, it exhibits a strong antiproliferative activity on all stages of development of the parasite by altering membrane integrity and potential. Hederacolchiside A1 shows antiproliferation activities in three cancer cell lines with the IC50 value of 2.4 uM, it exhibits a preferential cytotoxicity on a pigmented melanoma cell line. It suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K Akt mTOR signaling pathway.

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