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ERKs (Extracellular-signal-regulated kinases) are widely expressed protein kinase intracellular signalling molecules that are involved in functions including the regulation of meiosis, mitosis, and postmitotic functions in differentiated cells. Many different stimuli, including growth factors, cytokines, virus infection, ligands for heterotrimeric G protein-coupled receptors, transforming agents, and carcinogens, activate the ERK pathway. In the MAPK/ERK pathway, Ras activates c-Raf, followed by mitogen-activated protein kinase kinase (abbreviated as MKK, MEK, or MAP2K) and then MAPK1/2 (below). Ras is typically activated by growth hormones through receptor tyrosine kinases and GRB2/SOS, but may also receive other signals. ERKs are known to activate many transcription factors, such as ELK1, and some downstream protein kinases. Disruption of the ERK pathway is common in cancers, especially Ras, c-Raf and receptors such as HER2.
Albanol B is an arylbenzofuran derivative which can be isolated from mulberries. Albanol B exhibits anti-Alzheimer's disease, anti-bacterial and antioxidant activities. Albanol B inhibits cancer cells proliferation, down-regulates CDK1 expression. Albanol B also induces cell cycle arrest at G2/M and apoptosis. And Albanol B induces mitochondrial ROS production and increases the phosphorylation levels of AKT and ERK1/2.
Ophiopogonin D (Standard) is the analytical standard of Ophiopogonin D. This product is intended for research and analytical applications. Ophiopogonin D can be isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D can inhibit isteoclastic differentiation in RAW264.7 cells. Ophiopogonin D has protective effect as an antioxidant in H2O2-induced endothelial injury. Ophiopogonin D blocks ERK signaling cascades. Ophiopogonin D alleviates high-fat diet-induced metabolic syndrome and changes the structure of gut microbiota in mice. Ophiopogonin D has been used against inflammatory, metabolic and cardiovascular diseases.
26-Deoxyactein is a constituent isolated from Cimicifuga racemosa, prevents TCDD-induced osteoblasts damage. 26-Deoxyactein inhibits increased AhR, CYP1A1 and ERK levels.
Citropten (Standard) is the analytical standard of Citropten. This product is intended for research and analytical applications. Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
Salbutamol-d3 (Albuterol-d3) is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease.
Triphenyl phosphate-d15 is the deuterium labeled Triphenyl phosphate. Triphenyl phosphate is an orally active, blood-brain barrier-permeable aryl organophosphate flame retardant and endocrine disruptor. Triphenyl phosphate disrupts mitochondrial dynamic balance through oxidative stress, induces excessive mitophagy and apoptosis, and ultimately leads to myocardial fibrosis. In the brain, Triphenyl phosphate activates the NF-κB inflammatory pathway by disrupting the gut microbiota, alters tryptophan metabolism and elevates neurotoxins, thereby inducing anxiety- and depression-like behaviors. In the skeletal and reproductive systems, Triphenyl phosphate inhibits osteoblast differentiation and induces germ cell apoptosis by suppressing the MAPK/ERK pathway and activating the JNK signal, respectively. In adipose and placental tissues, Triphenyl phosphate promotes lipid accumulation by activating the PI3K/AKT-PPARγ axis, and disrupts placental metabolism via the MAOA/ROS/NF-κB cascade, impairing neurodevelopment of offspring.
SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders.
Prosaptide Tx14(A) TFA, a prosaposin-derived peptide, is a potent GPR37L1 and GPR37 agonist with EC50s of 5 and 7 nM, respectively. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells.
Fucoxanthin (Standard) is the analytical standard of Fucoxanthin. This product is intended for research and analytical applications. Fucoxanthin (all-trans-Fucoxanthin) is a marine carotenoid and shows anti-obesity, anti-diabetic, anti-oxidant, anti-inflammatory and anticancer activities.
18:0-22:6 DG (1-Stearoyl-2-docosahexaenoyl-sn-glycerol) is a diacylglycerol (DG) that can interact with RasGRP (Ras guanine nucleotide-releasing protein) (Ki = 8.37 μM) and modulate the activation of MAP kinases (such as ERK1/ERK2), which play a crucial role in cellular signaling processes. 18:0-22:6 DG can also activate protein kinase C (PKC) isozyme. 18:0-22:6 DG can be used for research of cancer, immunology and metabolic disease.
Citronellol (Standard) is the analytical standard of Citronellol. Citronellol (Standard) is an orally active inducer of apoptosis. Citronellol (Standard) can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol (Standard) can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol (Standard) can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol (Standard) exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.
Isoscopoletin (Standard) is the analytical standard of Isoscopoletin. This product is intended for research and analytical applications. Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC50s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively. Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitory activity against HBV replication. Isoscopoletin exhibits anti-inflammatory activity through inhibition of MAPK/NF-κB/STAT/AKT signaling pathway.
Salbutamol (Albuterol) hemisulfate (Standard) is the analytical standard of Salbutamol hemisulfate (HY-B0436). This product is intended for research and analytical applications. Salbutamol (Albuterol) hemisulfate is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol hemisulfate promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol hemisulfate can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease.
Peptide R analogue 10 (compound 10) is an analog of the CXCR4 antagonist peptide Peptide R (HY-P4111) with stronger antagonistic potency, specificity and plasma stability. Peptide R analogue 10 can inhibit CXCL12-mediated cell migration, ERK phosphorylation and CXCR4 internalization. Peptide R analogue 10 can be used in the study of CXCR4 overexpressing leukemia and colon cancer.
PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader (DC50 = 5.0 nM; Dmax ≥ 99%). PROTAC HPK1 Degrader-5 significantly inhibits SLP76 phosphorylation and enhanced ERK pathway activation through degrading HPK1, thereby stimulating IL-2 and IFN-γ release. PROTAC HPK1 Degrader-5 exhibits the ability to overcome the immunosuppressive effects imposed by PGE2, NECA or TGF-β. PROTAC HPK1 Degrader-5 alone efficaciously inhibits tumor growth in an MC38 syngeneic mouse model. PROTAC HPK1 Degrader-5 can be used for the study of tumor (such as colorectal cancer) immunotherapy (Pink: Target protein ligand (HY-175549); Blue: E3 ligand (HY-W023573); Black: Linker; E3 ligand + Linker (HY-175551)).
RANKL-IN-1 is a selective and orally active Receptor Activator of Nuclear Factor-κ B Ligand (RANKL) inhibitor with a KD value of 7.6 μM. RANKL-IN-1 exhibits inhibitory activity and selectivity against osteoclastogenesis with an IC50 value of 0.07 μM and SI of 82.57. RANKL-IN-1binds directly to RANKL and blocks the RANKL-induced activation of the NF-κB and MAPK pathways. RANKL-IN-1 can be used for the research of metabolic disease, such as osteoporosis.
c-Fos-IN-1 (Compound P16) is a c-Jun inhibitor, and decreases mRNA levels and protein levels of c-Fos. c-Fos-IN-1 also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. c-Fos-IN-1 shows anticancer activity by inhibiting ERK/c-Fos/Jun pathway. c-Fos-IN-1 inhibits the proliferation and migration of gastric cancer cells (IC50: 2.31 μM for MGC-803 cell). c-Fos-IN-1 arrests cell cycle at G2/M phase and induces cancer cell apoptosis. c-Fos-IN-1 inhibits gastric cancer tumor growth.
AG01 is a monoclonal antibody against progranulin (GP88). AG01 inhibits triple-negative breast cancer (TNBC) cell proliferation and migration, reduces the expression of phosphorylated protein kinases p-Src, p-AKT, and p-ERK, and reduces the expression of oncogenic proteins such as Axl, c-MET, HIF-1α, and VEGF. AG01 inhibits tumor growth and Ki67 expression in a TNBC xenograft mouse model. AG01 can be used in the research of TNBC and other cancers.
ERK-CLIPTAC is a ERKCLIPTAC (click chemistry-synthesized proteolysis-targeting chimera) degrader. ERK-CLIPTAC forms intracellularly via click chemistry from ERK1/2-IN-14 (HY-175578) and Tz-thalidomide (HY-101460). The formed ERK-CLIPTAC recruits the E3 ubiquitin ligase CRBN to ERK1/2, thereby inducing ubiquitination and subsequent degradation of ERK1/2. Due to its lack of cell permeability, ERK-CLIPTAC cannot induce ERK1/2 degradation in cells. ERK-CLIPTAC can be used in research related to melanoma and colorectal cancer.
Resolvin D5 is an anti-inflammatory and analgesic agent produced in M2 macrophages. Resolvin D5 alleviates Paclitaxel (HY-B0015)-induced mechanical allodynia and inflammatory pain by activating the GPR32 receptor, with gender specificity (effective only in male mice) and independence from TRPV1 or TRPA1 channels. Resolvin D5 attenuates LPS-induced ERK phosphorylation and NF-κB nuclear translocation, downregulates proinflammatory mediators such as IL-6 and CCL5, inhibits Th17 cell differentiation and osteoclastogenesis, promotes regulatory T cell differentiation, and shows no cytotoxicity to human monocytes. The level of Resolvin D5 is elevated in arthritic SKG mice, but Resolvin D5 has no effect on dendritic cell differentiation or M1 macrophage polarization, nor does it prevent ZyA-induced arthritis progression. Resolvin D5 is suitable for research related to chemotherapy-induced peripheral neuropathy, inflammatory pain and rheumatoid arthritis.
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