p-erk1/2

Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.

Mirdametinib (PD325901) is an MEK inhibitor (IC50=0.33 nM) with selective, non-ATP-competitive, and oral activity. Mirdametinib exhibits antitumor activity by inhibiting p-ERK1/2 expression and inducing apoptosis.

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1/2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

Carpaine is a natural product exhibiting antimalarial activity, with an approximate IC50 of 4μM against P. falciparum in NL20 cells. It demonstrates cardioprotective and anti-inflammatory effects by activating FAK, ERK1/2, and AKT pathways while inhibiting ROS production.

Bromuconazole is a triazole fungicide with oral efficacy and blood-brain barrier permeability. It offers protection to crops against various fungal contaminations. Bromuconazole is cytotoxic to multiple cancer cells, inducing G0/G1 phase cell cycle arrest and inhibiting DNA synthesis. It disrupts cytoskeletal structures, causes genotoxic damage, induces apoptosis, and leads to mitochondrial membrane depolarization. Bromuconazole activates caspase-3, triggers the excessive production of ROS, p53, and Bax, promotes lipid peroxidation, and increases the activity of SOD and CAT while downregulating Bcl-2. By upregulating p-ERK1/2 and p-JNK, it disrupts the MAPK signaling pathway, impairing the endometrial and trophoblast cell stress responses, which hinders implantation. Bromuconazole is used in research related to glioma, colon cancer, reproductive damage (implantation dysfunction), and cardiac dysfunction.

Autotaxin-IN-8 (Compound 14E) is an orally active inhibitor of Autotaxin, demonstrating an IC50 of 14.2 nM against hAutotaxin. It inhibits Autotaxin activity, suppresses MAPK activation, and reduces LPAR1 and p-ERK1/2 levels. Autotaxin-IN-8 also decreases the phosphorylation of JNK and p38. In a mouse model of pulmonary fibrosis, it reduces collagen deposition and is applicable for studies related to pulmonary fibrosis.

BRAFV600E/ABL2-IN-2 is a dual inhibitor targeting BRAFV600E and ABL2 kinases, with an IC50 of 0.088 μM for human-derived BRAFV600E and 0.3 μM for human-derived ABL2. It reduces phosphorylation levels of downstream ERK1/2 and CrkL in melanoma cells, decreases the expression of P-glycoprotein (P-glycoprotein), and induces G1 phase cell cycle arrest and apoptosis (Apoptosis) in melanoma cells. This compound is useful for research related to melanoma.

NFI23 is a GluN2B-NMDAR inhibitor with an IC50 of 1.31 μM and a Ki of 5.98 nM. It can cross the blood-brain barrier and binds to the ifenprodil binding site of GluN2B-NMDAR, reducing NMDA-induced Ca2+ influx and reactive oxygen species (ROS) production. It helps maintain mitochondrial membrane potential, inhibits neuronal apoptosis, and restores p-ERK1/2 expression. NFI23 demonstrates neuroprotective effects against NMDA-induced cytotoxicity and in a rat model of middle cerebral artery occlusion (MCAO), making it useful for ischemic stroke research.

Asperosaponin VI (Akebia saponin D) , the most abundant constituent of the rhizome of Dipsacus asper, has been used for the treatment of lower back pain, traumatic hematoma and bone fractures.

Ro 67-7476 is a positive allosteric modulator of mGluR1, which can enhance the calcium release induced by glutamate in HEK293 cells expressing rat mGluR1a. The EC50 is 60.1 nM. It is a P-ERK1/2 agonist, and can activate ERK1/2 phosphorylation without the addition of exogenous glutamate (EC50 = 163.3 nM).

Ganglioside GM1 asialo is a component of cellular lipid rafts and can be formed by the cleavage of the sialic acid residue from ganglioside GM1 by neuraminidase. Ganglioside GM1 asialo is a glycolipid receptor for P. aeruginosa flagellin and stimulates defensive responses in host cells, including extracellular ATP release, calcium mobilization, and ERK1/2 phosphorylation when stimulated by flagellin and an anti-ganglioside GM1 asialo antibody. The percentage of ganglioside GM1 asialo-positive natural killer (NK) and CD8+ T cells in lung is increased in a mouse model of respiratory syncytial virus (RSV) infection compared with healthy animals. Depletion of ganglioside GM1 asialo-positive NK and T cells reduces IFN-γ levels in the lung, reduces weight loss, and increases lung viral load in RSV-infected mice. Ganglioside GM1 asialo mixture contains ganglioside GM1 asialo molecular species with C18:1 and C20:1 sphingoid backbones.

ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s), targeting hGX with an IC50 of 80 nM. It efficiently inhibits the phosphorylation of ERK1/2 and p-38. sPLA2s, part of the disulfide-rich, Ca2+-dependent enzyme family, catalyze the hydrolysis of glycero-phospholipids at the sn-2 position, releasing a fatty acid and a lysophospholipid. ROC-0929 is promising for research on inflammation-related diseases.

EGFRT790M/L858R-IN-2 is a potent, selective inhibitor of EGFRT790M/L858R, exhibiting IC50 values of 3.5 nM for EGFRT790M/L858R and 1290 nM for EGFR WT. This compound effectively decreases the expression of p-EGFR, P-AKT, P-ERK1/2, and induces apoptosis as well as cell cycle arrest in the G1 phase, demonstrating anti-cancer activity [1].

VEGFR-2-IN-52 (compound 14d) serves as a powerful inhibitor of VEGFR-2, exhibiting an IC 50 of 191.1 nM. It effectively reduces the protein expression levels of p-VEGFR-2, MMP9, p-ERK1/2, and p-MEK1. In addition, VEGFR-2-IN-52 demonstrates cytotoxic properties by inducing apoptosis and arresting the cell cycle at the G0/G1 phase, and it enhances the levels of ROS.

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

Asperosaponin VI (Standard) is a reference standard for research and analysis in studies involving Asperosaponin VI. Asperosaponin VI (Akebia saponin D) , the most abundant constituent of the rhizome of Dipsacus asper, has been used for the treatment of lower back pain, traumatic hematoma and bone fractures.

2-Hydroxy-3-methylanthraquinone is a natural anthraquinone derivative that exhibits cytotoxic and pro-apoptotic activity against various tumor cells. It modulates SRC-related signaling and the activity of the IL-6/JAK2/STAT3 pathway, and induces a decrease in mitochondrial membrane potential and Caspase-3-dependent apoptosis. It can also influence MAPK-related signaling pathways, including the phosphorylation levels of p38MAPK and ERK1/2. 2-Hydroxy-3-methylanthraquinone is also commonly used in research related to anthraquinone chemistry, redox properties, and the pharmacological activity of natural products.

7-Oxo-beta-sitosterol (7-Ketositosterol), a phytosterol isolated from the fruit of x giganteus, has anticancer and antitumor activity, inhibits the proliferation of HL-60 acute myeloid leukemia (AML) cells, and stimulates the growth of HL-60 acute myeloid leukemia (AML) cells through the downregulation of the levels of S1P, p-44/42 ERK1/2 and p-NF-κB p65 proteins. -κB p65 protein levels to stimulate ceramide accumulation and apoptosis, and can be used to study breast cancer.